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Published in: Cancer Cell International 1/2005

Open Access 01-12-2005 | Review

ABC transporters as multidrug resistance mechanisms and the development of chemosensitizers for their reversal

Author: Cheol-Hee Choi

Published in: Cancer Cell International | Issue 1/2005

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Abstract

One of the major problems related with anticancer chemotherapy is resistance against anticancer drugs. The ATP-binding cassette (ABC) transporters are a family of transporter proteins that are responsible for drug resistance and a low bioavailability of drugs by pumping a variety of drugs out cells at the expense of ATP hydrolysis. One strategy for reversal of the resistance of tumor cells expressing ABC transporters is combined use of anticancer drugs with chemosensitizers. In this review, the physiological functions and structures of ABC transporters, and the development of chemosensitizers are described focusing on well-known proteins including P-glycoprotein, multidrug resistance associated protein, and breast cancer resistance protein.
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Literature
1.
go back to reference Stavrovskaya AA: Cellular mechanisms of multidrug resistance of tumor cells. Biochemistry (Mosc). 2000, 65: 95-106. Stavrovskaya AA: Cellular mechanisms of multidrug resistance of tumor cells. Biochemistry (Mosc). 2000, 65: 95-106.
2.
go back to reference Riordan JR, Ling V: Purification of P-glycoprotein from plasma membrane vesicles of Chinese hamster ovary cell mutants with reduced colchicine permeability. J Biol Chem. 1979, 254: 12701-12705.PubMed Riordan JR, Ling V: Purification of P-glycoprotein from plasma membrane vesicles of Chinese hamster ovary cell mutants with reduced colchicine permeability. J Biol Chem. 1979, 254: 12701-12705.PubMed
3.
go back to reference Di Pietro A, Dayan G, Conseil G, Steinfels E, Krell T, Trompier D, Baubichon-Cortay H, Jault J: P-glycoprotein-mediated resistance to chemotherapy in cancer cells: using recombinant cytosolic domains to establish structure-function relationships. Braz J Med Biol Res. 1999, 32: 925-939. 10.1590/S0100-879X1999000800001.PubMed Di Pietro A, Dayan G, Conseil G, Steinfels E, Krell T, Trompier D, Baubichon-Cortay H, Jault J: P-glycoprotein-mediated resistance to chemotherapy in cancer cells: using recombinant cytosolic domains to establish structure-function relationships. Braz J Med Biol Res. 1999, 32: 925-939. 10.1590/S0100-879X1999000800001.PubMed
4.
go back to reference Dean M, Hamon Y, Chimini G: The human ATP-binding cassette (ABC) transporter superfamily. J Lipid Res. 2001, 42: 1007-1017.PubMed Dean M, Hamon Y, Chimini G: The human ATP-binding cassette (ABC) transporter superfamily. J Lipid Res. 2001, 42: 1007-1017.PubMed
5.
go back to reference Efferth T: The human ATP-binding cassette transporter genes: from the bench to the bedside. Curr Mol Med. 2001, 1: 45-65. 10.2174/1566524013364194.PubMed Efferth T: The human ATP-binding cassette transporter genes: from the bench to the bedside. Curr Mol Med. 2001, 1: 45-65. 10.2174/1566524013364194.PubMed
6.
go back to reference Cole SP, Bhardwaj G, Gerlach JH, Mackie JE, Grant CE, Almquist KC, Stewart AJ, Kurz EU, Duncan AM, Deeley RG: Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science. 1992, 258: 1650-1654.PubMed Cole SP, Bhardwaj G, Gerlach JH, Mackie JE, Grant CE, Almquist KC, Stewart AJ, Kurz EU, Duncan AM, Deeley RG: Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science. 1992, 258: 1650-1654.PubMed
7.
go back to reference Doyle LA, Yang W, Abruzzo LV, Krogmann T, Gao Y, Rishi AK, Ross DD: A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci U S A. 1998, 95: 15665-15670. 10.1073/pnas.95.26.15665.PubMedCentralPubMed Doyle LA, Yang W, Abruzzo LV, Krogmann T, Gao Y, Rishi AK, Ross DD: A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc Natl Acad Sci U S A. 1998, 95: 15665-15670. 10.1073/pnas.95.26.15665.PubMedCentralPubMed
8.
go back to reference Maliepaard M, van Gastelen MA, de Jong LA, Pluim D, van Waardenburg RC, Ruevekamp-Helmers MC, Floot BG, Schellens JH: Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line. Cancer Res. 1999, 59: 4559-4563.PubMed Maliepaard M, van Gastelen MA, de Jong LA, Pluim D, van Waardenburg RC, Ruevekamp-Helmers MC, Floot BG, Schellens JH: Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line. Cancer Res. 1999, 59: 4559-4563.PubMed
9.
go back to reference Bell DR, Trent JM, Willard HF, Riordan JR, Ling V: Chromosomal location of human P-glycoprotein gene sequences. Cancer Genet Cytogenet. 1987, 25: 141-148. 10.1016/0165-4608(87)90169-5.PubMed Bell DR, Trent JM, Willard HF, Riordan JR, Ling V: Chromosomal location of human P-glycoprotein gene sequences. Cancer Genet Cytogenet. 1987, 25: 141-148. 10.1016/0165-4608(87)90169-5.PubMed
10.
go back to reference van Kuijck MA, Kool M, Merkx GF, Geurts van Kessel A, Bindels RJ, Deen PM, van Os CH: Assignment of the canalicular multispecific organic anion transporter gene (CMOAT) to human chromosome 10q24 and mouse chromosome 19D2 by fluorescent in situ hybridization. Cytogenet Cell Genet. 1997, 77: 285-287.PubMed van Kuijck MA, Kool M, Merkx GF, Geurts van Kessel A, Bindels RJ, Deen PM, van Os CH: Assignment of the canalicular multispecific organic anion transporter gene (CMOAT) to human chromosome 10q24 and mouse chromosome 19D2 by fluorescent in situ hybridization. Cytogenet Cell Genet. 1997, 77: 285-287.PubMed
11.
go back to reference Kool M, de Haas M, Scheffer GL, Scheper RJ, van Eijk MJ, Juijn JA, Baas F, Borst P: Analysis of expression of cMOAT (MRP2), MRP3, MRP4, and MRP5, homologues of the multidrug resistance-associated protein gene (MRP1), in human cancer cell lines. Cancer Res. 1997, 57: 3537-3547.PubMed Kool M, de Haas M, Scheffer GL, Scheper RJ, van Eijk MJ, Juijn JA, Baas F, Borst P: Analysis of expression of cMOAT (MRP2), MRP3, MRP4, and MRP5, homologues of the multidrug resistance-associated protein gene (MRP1), in human cancer cell lines. Cancer Res. 1997, 57: 3537-3547.PubMed
12.
go back to reference Kool M, van der Linden M, de Haas M, Baas F, Borst P: Expression of human MRP6, a homologue of the multidrug resistance protein gene MRP1, in tissues and cancer cells. Cancer Res. 1999, 59: 175-182.PubMed Kool M, van der Linden M, de Haas M, Baas F, Borst P: Expression of human MRP6, a homologue of the multidrug resistance protein gene MRP1, in tissues and cancer cells. Cancer Res. 1999, 59: 175-182.PubMed
13.
go back to reference Hopper E, Belinsky MG, Zeng H, Tosolini A, Testa JR, Kruh GD: Analysis of the structure and expression pattern of MRP7 (ABCC10), a new member of the MRP subfamily. Cancer Lett. 2001, 162: 181-191. 10.1016/S0304-3835(00)00646-7.PubMed Hopper E, Belinsky MG, Zeng H, Tosolini A, Testa JR, Kruh GD: Analysis of the structure and expression pattern of MRP7 (ABCC10), a new member of the MRP subfamily. Cancer Lett. 2001, 162: 181-191. 10.1016/S0304-3835(00)00646-7.PubMed
14.
go back to reference Bera TK, Lee S, Salvatore G, Lee B, Pastan I: MRP8, a new member of ABC transporter superfamily, identified by EST database mining and gene prediction program, is highly expressed in breast cancer. Mol Med. 2001, 7: 509-516.PubMedCentralPubMed Bera TK, Lee S, Salvatore G, Lee B, Pastan I: MRP8, a new member of ABC transporter superfamily, identified by EST database mining and gene prediction program, is highly expressed in breast cancer. Mol Med. 2001, 7: 509-516.PubMedCentralPubMed
15.
go back to reference Knutsen T, Rao VK, Ried T, Mickley L, Schneider E, Miyake K, Ghadimi BM, Padilla-Nash H, Pack S, Greenberger L, Cowan K, Dean M, Fojo T, Bates S: Amplification of 4q21-q22 and the MXR gene in independently derived mitoxantrone-resistant cell lines. Genes Chromosomes Cancer. 2000, 27: 110-116. 10.1002/(SICI)1098-2264(200001)27:1<110::AID-GCC14>3.0.CO;2-4.PubMed Knutsen T, Rao VK, Ried T, Mickley L, Schneider E, Miyake K, Ghadimi BM, Padilla-Nash H, Pack S, Greenberger L, Cowan K, Dean M, Fojo T, Bates S: Amplification of 4q21-q22 and the MXR gene in independently derived mitoxantrone-resistant cell lines. Genes Chromosomes Cancer. 2000, 27: 110-116. 10.1002/(SICI)1098-2264(200001)27:1<110::AID-GCC14>3.0.CO;2-4.PubMed
16.
go back to reference Hu K, Morris ME: Effects of benzyl-, phenethyl-, and alpha-naphthyl isothiocyanates on P-glycoprotein- and MRP1-mediated transport. J Pharm Sci. 2004, 93: 1901-1911. 10.1002/jps.20101.PubMed Hu K, Morris ME: Effects of benzyl-, phenethyl-, and alpha-naphthyl isothiocyanates on P-glycoprotein- and MRP1-mediated transport. J Pharm Sci. 2004, 93: 1901-1911. 10.1002/jps.20101.PubMed
17.
go back to reference Arora A, Seth K, Shukla Y: Reversal of P-glycoprotein-mediated multidrug resistance by diallyl sulfide in K562 leukemic cells and in mouse liver. Carcinogenesis. 2004, 25: 941-949. 10.1093/carcin/bgh060.PubMed Arora A, Seth K, Shukla Y: Reversal of P-glycoprotein-mediated multidrug resistance by diallyl sulfide in K562 leukemic cells and in mouse liver. Carcinogenesis. 2004, 25: 941-949. 10.1093/carcin/bgh060.PubMed
18.
go back to reference Walter RB, Raden BW, Cronk MR, Bernstein ID, Appelbaum FR, Banker DE: The peripheral benzodiazepine receptor ligand PK11195 overcomes different resistance mechanisms to sensitize AML cells to gemtuzumab ozogamicin. Blood. 2004, 103: 4276-4284. 10.1182/blood-2003-11-3825.PubMed Walter RB, Raden BW, Cronk MR, Bernstein ID, Appelbaum FR, Banker DE: The peripheral benzodiazepine receptor ligand PK11195 overcomes different resistance mechanisms to sensitize AML cells to gemtuzumab ozogamicin. Blood. 2004, 103: 4276-4284. 10.1182/blood-2003-11-3825.PubMed
19.
go back to reference Haus-Cohen M, Assaraf YG, Binyamin L, Benhar I, Reiter Y: Disruption of P-glycoprotein anticancer drug efflux activity by a small recombinant single-chain Fv antibody fragment targeted to an extracellular epitope. Int J Cancer. 2004, 109: 750-758. 10.1002/ijc.20037.PubMed Haus-Cohen M, Assaraf YG, Binyamin L, Benhar I, Reiter Y: Disruption of P-glycoprotein anticancer drug efflux activity by a small recombinant single-chain Fv antibody fragment targeted to an extracellular epitope. Int J Cancer. 2004, 109: 750-758. 10.1002/ijc.20037.PubMed
20.
go back to reference Ramachandran C, Rabi T, Fonseca HB, Melnick SJ, Escalon EA: Novel plant triterpenoid drug amooranin overcomes multidrug resistance in human leukemia and colon carcinoma cell lines. Int J Cancer. 2003, 105: 784-789. 10.1002/ijc.11180.PubMed Ramachandran C, Rabi T, Fonseca HB, Melnick SJ, Escalon EA: Novel plant triterpenoid drug amooranin overcomes multidrug resistance in human leukemia and colon carcinoma cell lines. Int J Cancer. 2003, 105: 784-789. 10.1002/ijc.11180.PubMed
21.
go back to reference Choi SU, Park SH, Kim KH, Choi EJ, Kim S, Park WK, Zhang YH, Kim HS, Jung NP, Lee CO: The bisbenzylisoquinoline alkaloids, tetrandine and fangchinoline, enhance the cytotoxicity of multidrug resistance-related drugs via modulation of P-glycoprotein. Anticancer Drugs. 1998, 9: 255-261.PubMed Choi SU, Park SH, Kim KH, Choi EJ, Kim S, Park WK, Zhang YH, Kim HS, Jung NP, Lee CO: The bisbenzylisoquinoline alkaloids, tetrandine and fangchinoline, enhance the cytotoxicity of multidrug resistance-related drugs via modulation of P-glycoprotein. Anticancer Drugs. 1998, 9: 255-261.PubMed
22.
go back to reference Kim SW, Kwon HY, Chi DW, Shim JH, Park JD, Lee YH, Pyo S, Rhee DK: Reversal of P-glycoprotein-mediated multidrug resistance by ginsenoside Rg(3). Biochem Pharmacol. 2003, 65: 75-82. 10.1016/S0006-2952(02)01446-6.PubMed Kim SW, Kwon HY, Chi DW, Shim JH, Park JD, Lee YH, Pyo S, Rhee DK: Reversal of P-glycoprotein-mediated multidrug resistance by ginsenoside Rg(3). Biochem Pharmacol. 2003, 65: 75-82. 10.1016/S0006-2952(02)01446-6.PubMed
23.
go back to reference Lee BH, Lee CO, Kwon MJ, Yi KY, Yoo SE, Choi SU: Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. Anticancer Drugs. 2003, 14: 175-181. 10.1097/00001813-200302000-00012.PubMed Lee BH, Lee CO, Kwon MJ, Yi KY, Yoo SE, Choi SU: Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity. Anticancer Drugs. 2003, 14: 175-181. 10.1097/00001813-200302000-00012.PubMed
24.
go back to reference Ketabi-Kiyanvash N, Weiss J, Haefeli WE, Mikus G: P-glycoprotein modulation by the designer drugs methylenedioxymethamphetamine, methylenedioxyethylamphetamine and paramethoxyamphetamine. Addict Biol. 2003, 8: 413-418. 10.1080/13556210310001646475.PubMed Ketabi-Kiyanvash N, Weiss J, Haefeli WE, Mikus G: P-glycoprotein modulation by the designer drugs methylenedioxymethamphetamine, methylenedioxyethylamphetamine and paramethoxyamphetamine. Addict Biol. 2003, 8: 413-418. 10.1080/13556210310001646475.PubMed
25.
go back to reference Choi CH, Kang G, Min YD: Reversal of P-glycoprotein-mediated multidrug resistance by protopanaxatriol ginsenosides from Korean red ginseng. Planta Med. 2003, 69: 235-240. 10.1055/s-2003-38483.PubMed Choi CH, Kang G, Min YD: Reversal of P-glycoprotein-mediated multidrug resistance by protopanaxatriol ginsenosides from Korean red ginseng. Planta Med. 2003, 69: 235-240. 10.1055/s-2003-38483.PubMed
26.
go back to reference Dupuis ML, Tombesi M, Sabatini M, Cianfriglia M: Differential effect of HIV-1 protease inhibitors on P-glycoprotein function in multidrug-resistant variants of the human CD4+ T lymphoblastoid CEM cell line. Chemotherapy. 2003, 49: 8-16. 10.1159/000069782.PubMed Dupuis ML, Tombesi M, Sabatini M, Cianfriglia M: Differential effect of HIV-1 protease inhibitors on P-glycoprotein function in multidrug-resistant variants of the human CD4+ T lymphoblastoid CEM cell line. Chemotherapy. 2003, 49: 8-16. 10.1159/000069782.PubMed
27.
go back to reference Nieth C, Priebsch A, Stege A, Lage H: Modulation of the classical multidrug resistance (MDR) phenotype by RNA interference (RNAi). FEBS Lett. 2003, 545: 144-150. 10.1016/S0014-5793(03)00523-4.PubMed Nieth C, Priebsch A, Stege A, Lage H: Modulation of the classical multidrug resistance (MDR) phenotype by RNA interference (RNAi). FEBS Lett. 2003, 545: 144-150. 10.1016/S0014-5793(03)00523-4.PubMed
28.
go back to reference Wu H, Hait WN, Yang JM: Small interfering RNA-induced suppression of MDR1 (P-glycoprotein) restores sensitivity to multidrug-resistant cancer cells. Cancer Res. 2003, 63: 1515-1519.PubMed Wu H, Hait WN, Yang JM: Small interfering RNA-induced suppression of MDR1 (P-glycoprotein) restores sensitivity to multidrug-resistant cancer cells. Cancer Res. 2003, 63: 1515-1519.PubMed
29.
go back to reference Brooks T, Minderman H, O'Loughlin KL, Pera P, Ojima I, Baer MR, Bernacki RJ: Taxane-based reversal agents modulate drug resistance mediated by P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Mol Cancer Ther. 2003, 2: 1195-1205.PubMed Brooks T, Minderman H, O'Loughlin KL, Pera P, Ojima I, Baer MR, Bernacki RJ: Taxane-based reversal agents modulate drug resistance mediated by P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein. Mol Cancer Ther. 2003, 2: 1195-1205.PubMed
30.
go back to reference Kawase M, Shah A, Gaveriya H, Motohashi N, Sakagami H, Varga A, Molnar J: 3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells. Bioorg Med Chem. 2002, 10: 1051-1055. 10.1016/S0968-0896(01)00363-7.PubMed Kawase M, Shah A, Gaveriya H, Motohashi N, Sakagami H, Varga A, Molnar J: 3,5-dibenzoyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells. Bioorg Med Chem. 2002, 10: 1051-1055. 10.1016/S0968-0896(01)00363-7.PubMed
31.
go back to reference Ganeshaguru K, Wickremasinghe RG, Jones DT, Gordon M, Hart SM, Virchis AE, Prentice HG, Hoffbrand AV, Man A, Champain K, Csermak K, Mehta AB: Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002, 87: 167-176.PubMed Ganeshaguru K, Wickremasinghe RG, Jones DT, Gordon M, Hart SM, Virchis AE, Prentice HG, Hoffbrand AV, Man A, Champain K, Csermak K, Mehta AB: Actions of the selective protein kinase C inhibitor PKC412 on B-chronic lymphocytic leukemia cells in vitro. Haematologica. 2002, 87: 167-176.PubMed
32.
go back to reference Qi J, Yang CZ, Wang CY, Wang SB, Yang M, Wang JH: Function and mechanism of pyronaridine: a new inhibitor of P-glycoprotein-mediated multidrug resistance. Acta Pharmacol Sin. 2002, 23: 544-550.PubMed Qi J, Yang CZ, Wang CY, Wang SB, Yang M, Wang JH: Function and mechanism of pyronaridine: a new inhibitor of P-glycoprotein-mediated multidrug resistance. Acta Pharmacol Sin. 2002, 23: 544-550.PubMed
33.
go back to reference Choi CH, Sun KH, An CS, Yoo JC, Hahm KS, Lee IH, Sohng JK, Kim YC: Reversal of P-glycoprotein-mediated multidrug resistance by 5,6,7,3',4'-pentamethoxyflavone (Sinensetin). Biochem Biophys Res Commun. 2002, 295: 832-840. 10.1016/S0006-291X(02)00755-6.PubMed Choi CH, Sun KH, An CS, Yoo JC, Hahm KS, Lee IH, Sohng JK, Kim YC: Reversal of P-glycoprotein-mediated multidrug resistance by 5,6,7,3',4'-pentamethoxyflavone (Sinensetin). Biochem Biophys Res Commun. 2002, 295: 832-840. 10.1016/S0006-291X(02)00755-6.PubMed
34.
go back to reference Murakami N, Sugimoto M, Morita M, Kobayashi M: Total synthesis of agosterol A: an MDR-modulator from a marine sponge. Chemistry. 2001, 7: 2663-2670. 10.1002/1521-3765(20010618)7:12<2663::AID-CHEM26630>3.0.CO;2-U.PubMed Murakami N, Sugimoto M, Morita M, Kobayashi M: Total synthesis of agosterol A: an MDR-modulator from a marine sponge. Chemistry. 2001, 7: 2663-2670. 10.1002/1521-3765(20010618)7:12<2663::AID-CHEM26630>3.0.CO;2-U.PubMed
35.
go back to reference Kataoka Y, Ishikawa M, Miura M, Takeshita M, Fujita R, Furusawa S, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of vinblastine resistance in human leukemic cells by haloperidol and dihydrohaloperidol. Biol Pharm Bull. 2001, 24: 612-617. 10.1248/bpb.24.612.PubMed Kataoka Y, Ishikawa M, Miura M, Takeshita M, Fujita R, Furusawa S, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of vinblastine resistance in human leukemic cells by haloperidol and dihydrohaloperidol. Biol Pharm Bull. 2001, 24: 612-617. 10.1248/bpb.24.612.PubMed
36.
go back to reference Barancik M, Bohacova V, Kvackajova J, Hudecova S, Krizanova O, Breier A: SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance. Eur J Pharm Sci. 2001, 14: 29-36. 10.1016/S0928-0987(01)00139-7.PubMed Barancik M, Bohacova V, Kvackajova J, Hudecova S, Krizanova O, Breier A: SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance. Eur J Pharm Sci. 2001, 14: 29-36. 10.1016/S0928-0987(01)00139-7.PubMed
37.
go back to reference Silva GL, Cui B, Chavez D, You M, Chai HB, Rasoanaivo P, Lynn SM, O'Neill MJ, Lewis JA, Besterman JM, Monks A, Farnsworth NR, Cordell GA, Pezzuto JM, Kinghorn AD: Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei. J Nat Prod. 2001, 64: 1514-1520. 10.1021/np010295+.PubMed Silva GL, Cui B, Chavez D, You M, Chai HB, Rasoanaivo P, Lynn SM, O'Neill MJ, Lewis JA, Besterman JM, Monks A, Farnsworth NR, Cordell GA, Pezzuto JM, Kinghorn AD: Modulation of the multidrug-resistance phenotype by new tropane alkaloid aromatic esters from Erythroxylum pervillei. J Nat Prod. 2001, 64: 1514-1520. 10.1021/np010295+.PubMed
38.
go back to reference Kurosawa K, Takahashi K, Tsuda E, Tomida A, Tsuruo T: Reversal of multidrug resistance by novel nitrophenyl pyrones, SNF4435C and D. Jpn J Cancer Res. 2001, 92: 1235-1241.PubMed Kurosawa K, Takahashi K, Tsuda E, Tomida A, Tsuruo T: Reversal of multidrug resistance by novel nitrophenyl pyrones, SNF4435C and D. Jpn J Cancer Res. 2001, 92: 1235-1241.PubMed
39.
go back to reference Zhu A, Wang X, Guo Z: Study of tea polyphenol as a reversal agent for carcinoma cell lines' multidrug resistance (study of TP as a MDR reversal agent). Nucl Med Biol. 2001, 28: 735-740. 10.1016/S0969-8051(00)90202-6.PubMed Zhu A, Wang X, Guo Z: Study of tea polyphenol as a reversal agent for carcinoma cell lines' multidrug resistance (study of TP as a MDR reversal agent). Nucl Med Biol. 2001, 28: 735-740. 10.1016/S0969-8051(00)90202-6.PubMed
40.
go back to reference Hayashi M, Koike K, Rho MC, Kuwano M, Kishiye T, Komiyama K: Reversal of P-glycoprotein associated multidrug resistance by new isoprenoid derivatives. Anticancer Drug Des. 2001, 16: 255-260.PubMed Hayashi M, Koike K, Rho MC, Kuwano M, Kishiye T, Komiyama K: Reversal of P-glycoprotein associated multidrug resistance by new isoprenoid derivatives. Anticancer Drug Des. 2001, 16: 255-260.PubMed
41.
go back to reference Ishikawa M, Fujita R, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of acquired resistance to doxorubicin in K562 human leukemia cells by astemizole. Biol Pharm Bull. 2000, 23: 112-115.PubMed Ishikawa M, Fujita R, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of acquired resistance to doxorubicin in K562 human leukemia cells by astemizole. Biol Pharm Bull. 2000, 23: 112-115.PubMed
42.
go back to reference Boyd RA, Stern RH, Stewart BH, Wu X, Reyner EL, Zegarac EA, Randinitis EJ, Whitfield L: Atorvastatin coadministration may increase digoxin concentrations by inhibition of intestinal P-glycoprotein-mediated secretion. J Clin Pharmacol. 2000, 40: 91-98. 10.1177/00912700022008612.PubMed Boyd RA, Stern RH, Stewart BH, Wu X, Reyner EL, Zegarac EA, Randinitis EJ, Whitfield L: Atorvastatin coadministration may increase digoxin concentrations by inhibition of intestinal P-glycoprotein-mediated secretion. J Clin Pharmacol. 2000, 40: 91-98. 10.1177/00912700022008612.PubMed
43.
go back to reference Rho MC, Hayashi M, Fukami A, Obata R, Sunazuka T, Tomoda H, Komiyama K, Omura S: Reversal of multidrug resistance by 7-O-benzoylpyripyropene A in multidrug-resistant tumor cells. J Antibiot (Tokyo). 2000, 53: 1201-1206. Rho MC, Hayashi M, Fukami A, Obata R, Sunazuka T, Tomoda H, Komiyama K, Omura S: Reversal of multidrug resistance by 7-O-benzoylpyripyropene A in multidrug-resistant tumor cells. J Antibiot (Tokyo). 2000, 53: 1201-1206.
44.
go back to reference Okumura H, Chen ZS, Sakou M, Sumizawa T, Furukawa T, Komatsu M, Ikeda R, Suzuki H, Hirota K, Aikou T, Akiyama SI: Reversal of P-glycoprotein and multidrug-resistance protein-mediated drug resistance in KB cells by 5-O-benzoylated taxinine K. Mol Pharmacol. 2000, 58: 1563-1569.PubMed Okumura H, Chen ZS, Sakou M, Sumizawa T, Furukawa T, Komatsu M, Ikeda R, Suzuki H, Hirota K, Aikou T, Akiyama SI: Reversal of P-glycoprotein and multidrug-resistance protein-mediated drug resistance in KB cells by 5-O-benzoylated taxinine K. Mol Pharmacol. 2000, 58: 1563-1569.PubMed
45.
go back to reference Wang L, Kitaichi K, Hui CS, Takagi K, Sakai M, Yokogawa K, Miyamoto KI, Hasegawa T: Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo. Clin Exp Pharmacol Physiol. 2000, 27: 587-593. 10.1046/j.1440-1681.2000.03308.x.PubMed Wang L, Kitaichi K, Hui CS, Takagi K, Sakai M, Yokogawa K, Miyamoto KI, Hasegawa T: Reversal of anticancer drug resistance by macrolide antibiotics in vitro and in vivo. Clin Exp Pharmacol Physiol. 2000, 27: 587-593. 10.1046/j.1440-1681.2000.03308.x.PubMed
46.
go back to reference Lavie Y, Harel-Orbital T, Gaffield W, Liscovitch M: Inhibitory effect of steroidal alkaloids on drug transport and multidrug resistance in human cancer cells. Anticancer Res. 2001, 21: 1189-1194.PubMed Lavie Y, Harel-Orbital T, Gaffield W, Liscovitch M: Inhibitory effect of steroidal alkaloids on drug transport and multidrug resistance in human cancer cells. Anticancer Res. 2001, 21: 1189-1194.PubMed
47.
go back to reference Shah A, Gaveriya H, Motohashi N, Kawase M, Saito S, Sakagami H, Satoh K, Tada Y, Solymosi A, Walfard K, Molnar J: 3,5-diacetyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells. Anticancer Res. 2000, 20: 373-377.PubMed Shah A, Gaveriya H, Motohashi N, Kawase M, Saito S, Sakagami H, Satoh K, Tada Y, Solymosi A, Walfard K, Molnar J: 3,5-diacetyl-1,4-dihydropyridines: synthesis and MDR reversal in tumor cells. Anticancer Res. 2000, 20: 373-377.PubMed
48.
go back to reference Kawase M, Saito S, Motohashi N: Chemistry and biological activity of new 3-benzazepines. Int J Antimicrob Agents. 2000, 14: 193-201. 10.1016/S0924-8579(99)00155-7.PubMed Kawase M, Saito S, Motohashi N: Chemistry and biological activity of new 3-benzazepines. Int J Antimicrob Agents. 2000, 14: 193-201. 10.1016/S0924-8579(99)00155-7.PubMed
49.
go back to reference Wang F, Jiang X, Yang DC, Elliott RL, Head JF: Doxorubicin-gallium-transferrin conjugate overcomes multidrug resistance: evidence for drug accumulation in the nucleus of drug resistant MCF-7/ADR cells. Anticancer Res. 2000, 20: 799-808.PubMed Wang F, Jiang X, Yang DC, Elliott RL, Head JF: Doxorubicin-gallium-transferrin conjugate overcomes multidrug resistance: evidence for drug accumulation in the nucleus of drug resistant MCF-7/ADR cells. Anticancer Res. 2000, 20: 799-808.PubMed
50.
go back to reference Miyake N, Fujita R, Ishikawa M, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of multidrug resistance in human leukemia K562 by tamolarizine, a novel calcium antagonist. Jpn J Pharmacol. 2000, 82: 265-268. 10.1254/jjp.82.265.PubMed Miyake N, Fujita R, Ishikawa M, Takayanagi M, Takayanagi Y, Sasaki K: Reversal of multidrug resistance in human leukemia K562 by tamolarizine, a novel calcium antagonist. Jpn J Pharmacol. 2000, 82: 265-268. 10.1254/jjp.82.265.PubMed
51.
go back to reference Shiraki N, Hamada A, Yasuda K, Fujii J, Arimori K, Nakano M: Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins. Biol Pharm Bull. 2000, 23: 1528-1531.PubMed Shiraki N, Hamada A, Yasuda K, Fujii J, Arimori K, Nakano M: Inhibitory effect of human immunodeficiency virus protease inhibitors on multidrug resistance transporter P-glycoproteins. Biol Pharm Bull. 2000, 23: 1528-1531.PubMed
52.
go back to reference Pauli-Magnus C, von Richter O, Burk O, Ziegler A, Mettang T, Eichelbaum M, Fromm MF: Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000, 293: 376-382.PubMed Pauli-Magnus C, von Richter O, Burk O, Ziegler A, Mettang T, Eichelbaum M, Fromm MF: Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000, 293: 376-382.PubMed
53.
go back to reference Newman MJ, Rodarte JC, Benbatoul KD, Romano SJ, Zhang C, Krane S, Moran EJ, Uyeda RT, Dixon R, Guns ES, Mayer LD: Discovery and characterization of OC144-093, a novel inhibitor of P-glycoprotein-mediated multidrug resistance. Cancer Res. 2000, 60: 2964-2972.PubMed Newman MJ, Rodarte JC, Benbatoul KD, Romano SJ, Zhang C, Krane S, Moran EJ, Uyeda RT, Dixon R, Guns ES, Mayer LD: Discovery and characterization of OC144-093, a novel inhibitor of P-glycoprotein-mediated multidrug resistance. Cancer Res. 2000, 60: 2964-2972.PubMed
54.
go back to reference van Zuylen L, Sparreboom A, van der Gaast A, van der Burg ME, van Beurden V, Bol CJ, Woestenborghs R, Palmer PA, Verweij J: The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel. Clin Cancer Res. 2000, 6: 1365-1371.PubMed van Zuylen L, Sparreboom A, van der Gaast A, van der Burg ME, van Beurden V, Bol CJ, Woestenborghs R, Palmer PA, Verweij J: The orally administered P-glycoprotein inhibitor R101933 does not alter the plasma pharmacokinetics of docetaxel. Clin Cancer Res. 2000, 6: 1365-1371.PubMed
55.
go back to reference Kobayashi J, Shigemori H, Hosoyama H, Chen Z, Akiyama S, Naito M, Tsuruo T: Multidrug resistance reversal activity of taxoids from Taxus cuspidata in KB-C2 and 2780AD cells. Jpn J Cancer Res. 2000, 91: 638-642.PubMed Kobayashi J, Shigemori H, Hosoyama H, Chen Z, Akiyama S, Naito M, Tsuruo T: Multidrug resistance reversal activity of taxoids from Taxus cuspidata in KB-C2 and 2780AD cells. Jpn J Cancer Res. 2000, 91: 638-642.PubMed
56.
go back to reference Evers R, Kool M, Smith AJ, van Deemter L, de Haas M, Borst P: Inhibitory effect of the reversal agents V-104, GF120918 and Pluronic L61 on MDR1 Pgp-, MRP1- and MRP2-mediated transport. Br J Cancer. 2000, 83: 366-374. 10.1054/bjoc.2000.1260.PubMedCentralPubMed Evers R, Kool M, Smith AJ, van Deemter L, de Haas M, Borst P: Inhibitory effect of the reversal agents V-104, GF120918 and Pluronic L61 on MDR1 Pgp-, MRP1- and MRP2-mediated transport. Br J Cancer. 2000, 83: 366-374. 10.1054/bjoc.2000.1260.PubMedCentralPubMed
57.
go back to reference Dintaman JM, Silverman JA: Inhibition of P-glycoprotein by D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). Pharm Res. 1999, 16: 1550-1556. 10.1023/A:1015000503629.PubMed Dintaman JM, Silverman JA: Inhibition of P-glycoprotein by D-alpha-tocopheryl polyethylene glycol 1000 succinate (TPGS). Pharm Res. 1999, 16: 1550-1556. 10.1023/A:1015000503629.PubMed
58.
go back to reference Wang FS, Kobayashi H, Liang KW, Holland JF, Ohnuma T: Retrovirus-mediated transfer of anti-MDR1 ribozymes fully restores chemosensitivity of P-glycoprotein-expressing human lymphoma cells. Hum Gene Ther. 1999, 10: 1185-1195. 10.1089/10430349950018175.PubMed Wang FS, Kobayashi H, Liang KW, Holland JF, Ohnuma T: Retrovirus-mediated transfer of anti-MDR1 ribozymes fully restores chemosensitivity of P-glycoprotein-expressing human lymphoma cells. Hum Gene Ther. 1999, 10: 1185-1195. 10.1089/10430349950018175.PubMed
59.
go back to reference Alexanian AR, Arutyunian NS: Reversal of drug resistance in sarcoma-45 by the new calmodulin antagonist--trihydrochloride of [1,2,5-trimethyl-4-phenyl-4-beta-[N-(beta-ethylamino)-N-4'-methoxybe nzy l]-ethylamino] piperidine (AR-2). Invest New Drugs. 1999, 17: 105-110. 10.1023/A:1006397014409.PubMed Alexanian AR, Arutyunian NS: Reversal of drug resistance in sarcoma-45 by the new calmodulin antagonist--trihydrochloride of [1,2,5-trimethyl-4-phenyl-4-beta-[N-(beta-ethylamino)-N-4'-methoxybe nzy l]-ethylamino] piperidine (AR-2). Invest New Drugs. 1999, 17: 105-110. 10.1023/A:1006397014409.PubMed
60.
go back to reference Jonsson O, Behnam-Motlagh P, Persson M, Henriksson R, Grankvist K: Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity. Biochem Pharmacol. 1999, 58: 1801-1806. 10.1016/S0006-2952(99)00262-2.PubMed Jonsson O, Behnam-Motlagh P, Persson M, Henriksson R, Grankvist K: Increase in doxorubicin cytotoxicity by carvedilol inhibition of P-glycoprotein activity. Biochem Pharmacol. 1999, 58: 1801-1806. 10.1016/S0006-2952(99)00262-2.PubMed
61.
go back to reference Siedlik PH, Olson SC, Yang BB, Stern RH: Erythromycin coadministration increases plasma atorvastatin concentrations. J Clin Pharmacol. 1999, 39: 501-504.PubMed Siedlik PH, Olson SC, Yang BB, Stern RH: Erythromycin coadministration increases plasma atorvastatin concentrations. J Clin Pharmacol. 1999, 39: 501-504.PubMed
62.
go back to reference Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999, 16: 408-414. 10.1023/A:1018877803319.PubMed Kim RB, Wandel C, Leake B, Cvetkovic M, Fromm MF, Dempsey PJ, Roden MM, Belas F, Chaudhary AK, Roden DM, Wood AJ, Wilkinson GR: Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999, 16: 408-414. 10.1023/A:1018877803319.PubMed
63.
go back to reference Rho MC, Toyoshima M, Hayashi M, Koyano T, Subramaniam G, Kam TS, Komiyama K: Reversal of multidrug resistance by kopsiflorine isolated from Kopsia dasyrachis. Planta Med. 1999, 65: 307-310. 10.1055/s-1999-13991.PubMed Rho MC, Toyoshima M, Hayashi M, Koyano T, Subramaniam G, Kam TS, Komiyama K: Reversal of multidrug resistance by kopsiflorine isolated from Kopsia dasyrachis. Planta Med. 1999, 65: 307-310. 10.1055/s-1999-13991.PubMed
64.
go back to reference Li J, Xu L, He K: [Modulation of multiple drug resistance by nomegestrol acetate and droloxifene in K562/A02]. Zhonghua Xue Ye Xue Za Zhi. 1999, 20: 288-291.PubMed Li J, Xu L, He K: [Modulation of multiple drug resistance by nomegestrol acetate and droloxifene in K562/A02]. Zhonghua Xue Ye Xue Za Zhi. 1999, 20: 288-291.PubMed
65.
go back to reference Vanhoefer U, Muller MR, Hilger RA, Lindtner B, Klaassen U, Schleucher N, Rustum YM, Seeber S, Harstrick A: Reversal of MDR1-associated resistance to topotecan by PAK-200S, a new dihydropyridine analogue, in human cancer cell lines. Br J Cancer. 1999, 81: 1304-1310. 10.1038/sj.bjc.6694384.PubMedCentralPubMed Vanhoefer U, Muller MR, Hilger RA, Lindtner B, Klaassen U, Schleucher N, Rustum YM, Seeber S, Harstrick A: Reversal of MDR1-associated resistance to topotecan by PAK-200S, a new dihydropyridine analogue, in human cancer cell lines. Br J Cancer. 1999, 81: 1304-1310. 10.1038/sj.bjc.6694384.PubMedCentralPubMed
66.
go back to reference Miller DW, Batrakova EV, Kabanov AV: Inhibition of multidrug resistance-associated protein (MRP) functional activity with pluronic block copolymers. Pharm Res. 1999, 16: 396-401. 10.1023/A:1018873702411.PubMed Miller DW, Batrakova EV, Kabanov AV: Inhibition of multidrug resistance-associated protein (MRP) functional activity with pluronic block copolymers. Pharm Res. 1999, 16: 396-401. 10.1023/A:1018873702411.PubMed
67.
go back to reference Sharom FJ, Yu X, Lu P, Liu R, Chu JW, Szabo K, Muller M, Hose CD, Monks A, Varadi A, Seprodi J, Sarkadi B: Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells. Biochem Pharmacol. 1999, 58: 571-586. 10.1016/S0006-2952(99)00139-2.PubMed Sharom FJ, Yu X, Lu P, Liu R, Chu JW, Szabo K, Muller M, Hose CD, Monks A, Varadi A, Seprodi J, Sarkadi B: Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells. Biochem Pharmacol. 1999, 58: 571-586. 10.1016/S0006-2952(99)00139-2.PubMed
68.
go back to reference Drewe J, Gutmann H, Fricker G, Torok M, Beglinger C, Huwyler J: HIV protease inhibitor ritonavir: a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833. Biochem Pharmacol. 1999, 57: 1147-1152. 10.1016/S0006-2952(99)00026-X.PubMed Drewe J, Gutmann H, Fricker G, Torok M, Beglinger C, Huwyler J: HIV protease inhibitor ritonavir: a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833. Biochem Pharmacol. 1999, 57: 1147-1152. 10.1016/S0006-2952(99)00026-X.PubMed
69.
go back to reference Plouzek CA, Ciolino HP, Clarke R, Yeh GC: Inhibition of P-glycoprotein activity and reversal of multidrug resistance in vitro by rosemary extract. Eur J Cancer. 1999, 35: 1541-1545. 10.1016/S0959-8049(99)00180-X.PubMed Plouzek CA, Ciolino HP, Clarke R, Yeh GC: Inhibition of P-glycoprotein activity and reversal of multidrug resistance in vitro by rosemary extract. Eur J Cancer. 1999, 35: 1541-1545. 10.1016/S0959-8049(99)00180-X.PubMed
70.
go back to reference Xu JY, Zhou Q, Shen P, Tang W: Reversal effect of TTD on human multidrug resistant KBV200 cell line. J Exp Clin Cancer Res. 1999, 18: 549-552.PubMed Xu JY, Zhou Q, Shen P, Tang W: Reversal effect of TTD on human multidrug resistant KBV200 cell line. J Exp Clin Cancer Res. 1999, 18: 549-552.PubMed
71.
go back to reference Roe M, Folkes A, Ashworth P, Brumwell J, Chima L, Hunjan S, Pretswell I, Dangerfield W, Ryder H, Charlton P: Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives. Bioorg Med Chem Lett. 1999, 9: 595-600. 10.1016/S0960-894X(99)00030-X.PubMed Roe M, Folkes A, Ashworth P, Brumwell J, Chima L, Hunjan S, Pretswell I, Dangerfield W, Ryder H, Charlton P: Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives. Bioorg Med Chem Lett. 1999, 9: 595-600. 10.1016/S0960-894X(99)00030-X.PubMed
72.
go back to reference Chou TC, Depew KM, Zheng YH, Safer ML, Chan D, Helfrich B, Zatorska D, Zatorski A, Bornmann W, Danishefsky SJ: Reversal of anticancer multidrug resistance by the ardeemins. Proc Natl Acad Sci U S A. 1998, 95: 8369-8374. 10.1073/pnas.95.14.8369.PubMedCentralPubMed Chou TC, Depew KM, Zheng YH, Safer ML, Chan D, Helfrich B, Zatorska D, Zatorski A, Bornmann W, Danishefsky SJ: Reversal of anticancer multidrug resistance by the ardeemins. Proc Natl Acad Sci U S A. 1998, 95: 8369-8374. 10.1073/pnas.95.14.8369.PubMedCentralPubMed
73.
go back to reference Mendez-Vidal C, Quesada AR: Reversal of P-glycoprotein-mediated multidrug resistance in vitro by AV200, a new ardeemin derivative. Cancer Lett. 1998, 132: 45-50. 10.1016/S0304-3835(98)00156-6.PubMed Mendez-Vidal C, Quesada AR: Reversal of P-glycoprotein-mediated multidrug resistance in vitro by AV200, a new ardeemin derivative. Cancer Lett. 1998, 132: 45-50. 10.1016/S0304-3835(98)00156-6.PubMed
74.
go back to reference Sako M, Suzuki H, Hirota K: Syntheses of taxuspine C derivatives as functional inhibitors of P-glycoprotein, an ATP-associated cell-membrane transporter. Chem Pharm Bull (Tokyo). 1998, 46: 1135-1139. Sako M, Suzuki H, Hirota K: Syntheses of taxuspine C derivatives as functional inhibitors of P-glycoprotein, an ATP-associated cell-membrane transporter. Chem Pharm Bull (Tokyo). 1998, 46: 1135-1139.
75.
go back to reference Orlowski S, Valente D, Garrigos M, Ezan E: Bromocriptine modulates P-glycoprotein function. Biochem Biophys Res Commun. 1998, 244: 481-488. 10.1006/bbrc.1998.8289.PubMed Orlowski S, Valente D, Garrigos M, Ezan E: Bromocriptine modulates P-glycoprotein function. Biochem Biophys Res Commun. 1998, 244: 481-488. 10.1006/bbrc.1998.8289.PubMed
76.
go back to reference Hosoi E, Hirose M, Hamano S, Morimoto M, Kuroda Y: Effect of MDR antagonists on the cidal activity of vincristine for cells expressing MDR-1 is superior to those expressing MRP. Int J Oncol. 1998, 13: 343-348.PubMed Hosoi E, Hirose M, Hamano S, Morimoto M, Kuroda Y: Effect of MDR antagonists on the cidal activity of vincristine for cells expressing MDR-1 is superior to those expressing MRP. Int J Oncol. 1998, 13: 343-348.PubMed
77.
go back to reference Nussler V, Pelka-Fleisc R, Gieseler F, Hasmann M, Loser R, Gullis E, Stotzer O, Zwierzina H, Wilmanns W: In vitro efficacy of known P-glycoprotein modulators compared to droloxifene E and Z: studies on a human T-cell leukemia cell line and their resistant variants. Leuk Lymphoma. 1998, 31: 589-597.PubMed Nussler V, Pelka-Fleisc R, Gieseler F, Hasmann M, Loser R, Gullis E, Stotzer O, Zwierzina H, Wilmanns W: In vitro efficacy of known P-glycoprotein modulators compared to droloxifene E and Z: studies on a human T-cell leukemia cell line and their resistant variants. Leuk Lymphoma. 1998, 31: 589-597.PubMed
78.
go back to reference Naito S, Koike K, Ono M, Machida T, Tasaka S, Kiue A, Koga H, Kumazawa J: Development of novel reversal agents, imidazothiazole derivatives, targeting MDR1- and MRP-mediated multidrug resistance. Oncol Res. 1998, 10: 123-132.PubMed Naito S, Koike K, Ono M, Machida T, Tasaka S, Kiue A, Koga H, Kumazawa J: Development of novel reversal agents, imidazothiazole derivatives, targeting MDR1- and MRP-mediated multidrug resistance. Oncol Res. 1998, 10: 123-132.PubMed
79.
go back to reference Choudhuri SK, Chatterjee A: Reversal of resistance against doxorubicin by a newly developed compound, oxalyl bis(N-phenyl)hydroxamic acid in vitro. Anticancer Drugs. 1998, 9: 825-832.PubMed Choudhuri SK, Chatterjee A: Reversal of resistance against doxorubicin by a newly developed compound, oxalyl bis(N-phenyl)hydroxamic acid in vitro. Anticancer Drugs. 1998, 9: 825-832.PubMed
80.
go back to reference Baggetto LG, Dong M, Bernaud J, Espinosa L, Rigal D, Bonvallet R, Marthinet E: In vitro and in vivo reversal of cancer cell multidrug resistance by the semi-synthetic antibiotic tiamulin. Biochem Pharmacol. 1998, 56: 1219-1228. 10.1016/S0006-2952(98)00229-9.PubMed Baggetto LG, Dong M, Bernaud J, Espinosa L, Rigal D, Bonvallet R, Marthinet E: In vitro and in vivo reversal of cancer cell multidrug resistance by the semi-synthetic antibiotic tiamulin. Biochem Pharmacol. 1998, 56: 1219-1228. 10.1016/S0006-2952(98)00229-9.PubMed
81.
go back to reference Dale IL, Tuffley W, Callaghan R, Holmes JA, Martin K, Luscombe M, Mistry P, Ryder H, Stewart AJ, Charlton P, Twentyman PR, Bevan P: Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br J Cancer. 1998, 78: 885-892.PubMedCentralPubMed Dale IL, Tuffley W, Callaghan R, Holmes JA, Martin K, Luscombe M, Mistry P, Ryder H, Stewart AJ, Charlton P, Twentyman PR, Bevan P: Reversal of P-glycoprotein-mediated multidrug resistance by XR9051, a novel diketopiperazine derivative. Br J Cancer. 1998, 78: 885-892.PubMedCentralPubMed
82.
go back to reference Germann UA, Shlyakhter D, Mason VS, Zelle RE, Duffy JP, Galullo V, Armistead DM, Saunders JO, Boger J, Harding MW: Cellular and biochemical characterization of VX-710 as a chemosensitizer: reversal of P-glycoprotein-mediated multidrug resistance in vitro. Anticancer Drugs. 1997, 8: 125-140.PubMed Germann UA, Shlyakhter D, Mason VS, Zelle RE, Duffy JP, Galullo V, Armistead DM, Saunders JO, Boger J, Harding MW: Cellular and biochemical characterization of VX-710 as a chemosensitizer: reversal of P-glycoprotein-mediated multidrug resistance in vitro. Anticancer Drugs. 1997, 8: 125-140.PubMed
83.
go back to reference Rowinsky EK, Smith L, Wang YM, Chaturvedi P, Villalona M, Campbell E, Aylesworth C, Eckhardt SG, Hammond L, Kraynak M, Drengler R, Stephenson J, Harding MW, Von Hoff DD: Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP. J Clin Oncol. 1998, 16: 2964-2976.PubMed Rowinsky EK, Smith L, Wang YM, Chaturvedi P, Villalona M, Campbell E, Aylesworth C, Eckhardt SG, Hammond L, Kraynak M, Drengler R, Stephenson J, Harding MW, Von Hoff DD: Phase I and pharmacokinetic study of paclitaxel in combination with biricodar, a novel agent that reverses multidrug resistance conferred by overexpression of both MDR1 and MRP. J Clin Oncol. 1998, 16: 2964-2976.PubMed
84.
go back to reference Miao ZH, Li XT, Zhu YJ: [Reversal of multidrug resistance by cyproheptadine in KBV200 cells]. Yao Xue Xue Bao. 1997, 32: 321-325.PubMed Miao ZH, Li XT, Zhu YJ: [Reversal of multidrug resistance by cyproheptadine in KBV200 cells]. Yao Xue Xue Bao. 1997, 32: 321-325.PubMed
85.
go back to reference Greenberger LM, Collins KI, Annable T, Boni JP, May MK, Lai FM, Kramer R, Citeralla RV, Hallett WA, Powell D: alpha-(3,4-dimethyoxyphenyl)-3,4-dihydro-6,7-dimethoxy-alpha- [(4-methylphenyl)thio]-2(1H)-isoquinolineheptanenitrile (CL 329,753): a novel chemosensitizing agent for P-glycoprotein-mediated resistance with improved biological properties compared with verapamil and cyclosporine A. Oncol Res. 1996, 8: 207-218.PubMed Greenberger LM, Collins KI, Annable T, Boni JP, May MK, Lai FM, Kramer R, Citeralla RV, Hallett WA, Powell D: alpha-(3,4-dimethyoxyphenyl)-3,4-dihydro-6,7-dimethoxy-alpha- [(4-methylphenyl)thio]-2(1H)-isoquinolineheptanenitrile (CL 329,753): a novel chemosensitizing agent for P-glycoprotein-mediated resistance with improved biological properties compared with verapamil and cyclosporine A. Oncol Res. 1996, 8: 207-218.PubMed
86.
go back to reference Christensen JG, LeBlanc GA: Reversal of multidrug resistance in vivo by dietary administration of the phytochemical indole-3-carbinol. Cancer Res. 1996, 56: 574-581.PubMed Christensen JG, LeBlanc GA: Reversal of multidrug resistance in vivo by dietary administration of the phytochemical indole-3-carbinol. Cancer Res. 1996, 56: 574-581.PubMed
87.
go back to reference Kurosawa M, Okabe M, Hara N, Kawamura K, Suzuki S, Sakurada K, Asaka M: Reversal effect of itraconazole on adriamycin and etoposide resistance in human leukemia cells. Ann Hematol. 1996, 72: 17-21.PubMed Kurosawa M, Okabe M, Hara N, Kawamura K, Suzuki S, Sakurada K, Asaka M: Reversal effect of itraconazole on adriamycin and etoposide resistance in human leukemia cells. Ann Hematol. 1996, 72: 17-21.PubMed
88.
go back to reference Dantzig AH, Shepard RL, Cao J, Law KL, Ehlhardt WJ, Baughman TM, Bumol TF, Starling JJ: Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996, 56: 4171-4179.PubMed Dantzig AH, Shepard RL, Cao J, Law KL, Ehlhardt WJ, Baughman TM, Bumol TF, Starling JJ: Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996, 56: 4171-4179.PubMed
89.
go back to reference Claudio JA, Emerman JT: The effects of cyclosporin A, tamoxifen, and medroxyprogesterone acetate on the enhancement of adriamycin cytotoxicity in primary cultures of human breast epithelial cells. Breast Cancer Res Treat. 1996, 41: 111-122. 10.1007/BF01807156.PubMed Claudio JA, Emerman JT: The effects of cyclosporin A, tamoxifen, and medroxyprogesterone acetate on the enhancement of adriamycin cytotoxicity in primary cultures of human breast epithelial cells. Breast Cancer Res Treat. 1996, 41: 111-122. 10.1007/BF01807156.PubMed
90.
go back to reference Riffkin CD, Chung R, Wall DM, Zalcberg JR, Cowman AF, Foley M, Tilley L: Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine. Biochem Pharmacol. 1996, 52: 1545-1552. 10.1016/S0006-2952(96)00556-4.PubMed Riffkin CD, Chung R, Wall DM, Zalcberg JR, Cowman AF, Foley M, Tilley L: Modulation of the function of human MDR1 P-glycoprotein by the antimalarial drug mefloquine. Biochem Pharmacol. 1996, 52: 1545-1552. 10.1016/S0006-2952(96)00556-4.PubMed
91.
go back to reference Fardel O, Courtois A, Drenou B, Lamy T, Lecureur V, le Prise PY, Fauchet R: Inhibition of P-glycoprotein activity in human leukemic cells by mifepristone. Anticancer Drugs. 1996, 7: 671-677.PubMed Fardel O, Courtois A, Drenou B, Lamy T, Lecureur V, le Prise PY, Fauchet R: Inhibition of P-glycoprotein activity in human leukemic cells by mifepristone. Anticancer Drugs. 1996, 7: 671-677.PubMed
92.
go back to reference Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996, 49: 311-318.PubMed Schuetz EG, Beck WT, Schuetz JD: Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol. 1996, 49: 311-318.PubMed
93.
go back to reference Hu YP, Robert J: Azelastine and flezelastine as reversing agents of multidrug resistance: pharmacological and molecular studies. Biochem Pharmacol. 1995, 50: 169-175. 10.1016/0006-2952(95)02055-1.PubMed Hu YP, Robert J: Azelastine and flezelastine as reversing agents of multidrug resistance: pharmacological and molecular studies. Biochem Pharmacol. 1995, 50: 169-175. 10.1016/0006-2952(95)02055-1.PubMed
94.
go back to reference Borchers C, Ulrich WR, Klemm K, Ise W, Gekeler V, Haas S, Schodl A, Conrad J, Przybylski M, Boer R: B9209-005, an azido derivative of the chemosensitizer dexniguldipine-HCl, photolabels P-glycoprotein. Mol Pharmacol. 1995, 48: 21-29.PubMed Borchers C, Ulrich WR, Klemm K, Ise W, Gekeler V, Haas S, Schodl A, Conrad J, Przybylski M, Boer R: B9209-005, an azido derivative of the chemosensitizer dexniguldipine-HCl, photolabels P-glycoprotein. Mol Pharmacol. 1995, 48: 21-29.PubMed
95.
go back to reference Hofmann J, Gekeler V, Ise W, Noller A, Mitterdorfer J, Hofer S, Utz I, Gotwald M, Boer R, Glossmann H: Mechanism of action of dexniguldipine-HCl (B8509-035), a new potent modulator of multidrug resistance. Biochem Pharmacol. 1995, 49: 603-609. 10.1016/0006-2952(94)00479-6.PubMed Hofmann J, Gekeler V, Ise W, Noller A, Mitterdorfer J, Hofer S, Utz I, Gotwald M, Boer R, Glossmann H: Mechanism of action of dexniguldipine-HCl (B8509-035), a new potent modulator of multidrug resistance. Biochem Pharmacol. 1995, 49: 603-609. 10.1016/0006-2952(94)00479-6.PubMed
96.
go back to reference Thurlimann B, Kroger N, Greiner J, Mross K, Schuller J, Schernhammer E, Schumacher K, Gastl G, Hartlapp J, Kupper H: Dexverapamil to overcome epirubicin resistance in advanced breast cancer. J Cancer Res Clin Oncol. 1995, 121 (Suppl 3): R3-6.PubMed Thurlimann B, Kroger N, Greiner J, Mross K, Schuller J, Schernhammer E, Schumacher K, Gastl G, Hartlapp J, Kupper H: Dexverapamil to overcome epirubicin resistance in advanced breast cancer. J Cancer Res Clin Oncol. 1995, 121 (Suppl 3): R3-6.PubMed
97.
go back to reference Hirsch-Ernst KI, Ziemann C, Schmitz-Salue C, Foth H, Kahl GF: Modulation of P-glycoprotein and mdr1b mRNA expression by growth factors in primary rat hepatocyte culture. Biochem Biophys Res Commun. 1995, 215: 179-185. 10.1006/bbrc.1995.2450.PubMed Hirsch-Ernst KI, Ziemann C, Schmitz-Salue C, Foth H, Kahl GF: Modulation of P-glycoprotein and mdr1b mRNA expression by growth factors in primary rat hepatocyte culture. Biochem Biophys Res Commun. 1995, 215: 179-185. 10.1006/bbrc.1995.2450.PubMed
98.
go back to reference Kim SH, Yeo GS, Lim YS, Kang CD, Kim CM, Chung BS: Suppression of multidrug resistance via inhibition of heat shock factor by quercetin in MDR cells. Exp Mol Med. 1998, 30: 87-92.PubMed Kim SH, Yeo GS, Lim YS, Kang CD, Kim CM, Chung BS: Suppression of multidrug resistance via inhibition of heat shock factor by quercetin in MDR cells. Exp Mol Med. 1998, 30: 87-92.PubMed
99.
go back to reference Tsuruo T: [MDR reversing drugs for clinical development]. Gan To Kagaku Ryoho. 1994, 21: 962-967.PubMed Tsuruo T: [MDR reversing drugs for clinical development]. Gan To Kagaku Ryoho. 1994, 21: 962-967.PubMed
100.
go back to reference Breier A, Barancik M, Stefankova Z, Uhrik B, Tribulova N: Effect of pentoxifylline on P-glycoprotein mediated vincristine resistance of L1210 mouse leukemic cell line. Neoplasma. 1994, 41: 297-303.PubMed Breier A, Barancik M, Stefankova Z, Uhrik B, Tribulova N: Effect of pentoxifylline on P-glycoprotein mediated vincristine resistance of L1210 mouse leukemic cell line. Neoplasma. 1994, 41: 297-303.PubMed
101.
go back to reference Wigler PW, Patterson FK: Reversal agent inhibition of the multidrug resistance pump in human leukemic lymphoblasts. Biochim Biophys Acta. 1994, 1189: 1-6.PubMed Wigler PW, Patterson FK: Reversal agent inhibition of the multidrug resistance pump in human leukemic lymphoblasts. Biochim Biophys Acta. 1994, 1189: 1-6.PubMed
102.
go back to reference Gruol DJ, Zee MC, Trotter J, Bourgeois S: Reversal of multidrug resistance by RU 486. Cancer Res. 1994, 54: 3088-3091.PubMed Gruol DJ, Zee MC, Trotter J, Bourgeois S: Reversal of multidrug resistance by RU 486. Cancer Res. 1994, 54: 3088-3091.PubMed
103.
go back to reference Ganapathi R, Hercbergs A, Grabowski D, Ford J: Selective enhancement of vincristine cytotoxicity in multidrug-resistant tumor cells by dilantin (phenytoin). Cancer Res. 1993, 53: 3262-3265.PubMed Ganapathi R, Hercbergs A, Grabowski D, Ford J: Selective enhancement of vincristine cytotoxicity in multidrug-resistant tumor cells by dilantin (phenytoin). Cancer Res. 1993, 53: 3262-3265.PubMed
104.
go back to reference Hyafil F, Vergely C, Du Vignaud P, Grand-Perret T: In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 1993, 53: 4595-4602.PubMed Hyafil F, Vergely C, Du Vignaud P, Grand-Perret T: In vitro and in vivo reversal of multidrug resistance by GF120918, an acridonecarboxamide derivative. Cancer Res. 1993, 53: 4595-4602.PubMed
105.
go back to reference Callaghan R, Riordan JR: Synthetic and natural opiates interact with P-glycoprotein in multidrug-resistant cells. J Biol Chem. 1993, 268: 16059-16064.PubMed Callaghan R, Riordan JR: Synthetic and natural opiates interact with P-glycoprotein in multidrug-resistant cells. J Biol Chem. 1993, 268: 16059-16064.PubMed
106.
go back to reference Efferth T, Volm M: Modulation of P-glycoprotein-mediated multidrug resistance by monoclonal antibodies, immunotoxins or antisense oligodeoxynucleotides in kidney carcinoma and normal kidney cells. Oncology. 1993, 50: 303-308.PubMed Efferth T, Volm M: Modulation of P-glycoprotein-mediated multidrug resistance by monoclonal antibodies, immunotoxins or antisense oligodeoxynucleotides in kidney carcinoma and normal kidney cells. Oncology. 1993, 50: 303-308.PubMed
107.
go back to reference Kirk J, Houlbrook S, Stuart NS, Stratford IJ, Harris AL, Carmichael J: Selective reversal of vinblastine resistance in multidrug-resistant cell lines by tamoxifen, toremifene and their metabolites. Eur J Cancer. 1993, 29A: 1152-1157.PubMed Kirk J, Houlbrook S, Stuart NS, Stratford IJ, Harris AL, Carmichael J: Selective reversal of vinblastine resistance in multidrug-resistant cell lines by tamoxifen, toremifene and their metabolites. Eur J Cancer. 1993, 29A: 1152-1157.PubMed
108.
go back to reference Miyamoto K, Wakusawa S, Inoko K, Takagi K, Koyama M: Reversal of vinblastine resistance by a new staurosporine derivative, NA-382, in P388/ADR cells. Cancer Lett. 1992, 64: 177-183. 10.1016/0304-3835(92)90079-B.PubMed Miyamoto K, Wakusawa S, Inoko K, Takagi K, Koyama M: Reversal of vinblastine resistance by a new staurosporine derivative, NA-382, in P388/ADR cells. Cancer Lett. 1992, 64: 177-183. 10.1016/0304-3835(92)90079-B.PubMed
109.
go back to reference van Kalken CK, van der Hoeven JJ, de Jong J, Giaccone G, Schuurhuis GJ, Maessen PA, Blokhuis WM, van der Vijgh WJ, Pinedo HM: Bepridil in combination with anthracyclines to reverse anthracycline resistance in cancer patients. Eur J Cancer. 1991, 27: 739-744.PubMed van Kalken CK, van der Hoeven JJ, de Jong J, Giaccone G, Schuurhuis GJ, Maessen PA, Blokhuis WM, van der Vijgh WJ, Pinedo HM: Bepridil in combination with anthracyclines to reverse anthracycline resistance in cancer patients. Eur J Cancer. 1991, 27: 739-744.PubMed
110.
go back to reference Boesch D, Gaveriaux C, Jachez B, Pourtier-Manzanedo A, Bollinger P, Loor F: In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res. 1991, 51: 4226-4233.PubMed Boesch D, Gaveriaux C, Jachez B, Pourtier-Manzanedo A, Bollinger P, Loor F: In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res. 1991, 51: 4226-4233.PubMed
111.
go back to reference Friche E, Jensen PB, Sehested M, Demant EJ, Nissen NN: The solvents cremophor EL and Tween 80 modulate daunorubicin resistance in the multidrug resistant Ehrlich ascites tumor. Cancer Commun. 1990, 2: 297-303.PubMed Friche E, Jensen PB, Sehested M, Demant EJ, Nissen NN: The solvents cremophor EL and Tween 80 modulate daunorubicin resistance in the multidrug resistant Ehrlich ascites tumor. Cancer Commun. 1990, 2: 297-303.PubMed
112.
go back to reference Gosland MP, Lum BL, Sikic BI: Reversal by cefoperazone of resistance to etoposide, doxorubicin, and vinblastine in multidrug resistant human sarcoma cells. Cancer Res. 1989, 49: 6901-6905.PubMed Gosland MP, Lum BL, Sikic BI: Reversal by cefoperazone of resistance to etoposide, doxorubicin, and vinblastine in multidrug resistant human sarcoma cells. Cancer Res. 1989, 49: 6901-6905.PubMed
113.
go back to reference Ford JM, Prozialeck WC, Hait WN: Structural features determining activity of phenothiazines and related drugs for inhibition of cell growth and reversal of multidrug resistance. Mol Pharmacol. 1989, 35: 105-115.PubMed Ford JM, Prozialeck WC, Hait WN: Structural features determining activity of phenothiazines and related drugs for inhibition of cell growth and reversal of multidrug resistance. Mol Pharmacol. 1989, 35: 105-115.PubMed
114.
go back to reference Sato S, Watanabe Y, Okamura K, Hamanaka R, Mori T, Kohno K, Kuwano M: Potentiation of vincristine and actinomycin D by a new synthetic imidazole anti-tumor agent YM534 active against human cancer cells and multidrug-resistant cells. Anticancer Drug Des. 1989, 4: 125-135.PubMed Sato S, Watanabe Y, Okamura K, Hamanaka R, Mori T, Kohno K, Kuwano M: Potentiation of vincristine and actinomycin D by a new synthetic imidazole anti-tumor agent YM534 active against human cancer cells and multidrug-resistant cells. Anticancer Drug Des. 1989, 4: 125-135.PubMed
115.
go back to reference Cornwell MM, Pastan I, Gottesman MM: Certain calcium channel blockers bind specifically to multidrug-resistant human KB carcinoma membrane vesicles and inhibit drug binding to P-glycoprotein. J Biol Chem. 1987, 262: 2166-2170.PubMed Cornwell MM, Pastan I, Gottesman MM: Certain calcium channel blockers bind specifically to multidrug-resistant human KB carcinoma membrane vesicles and inhibit drug binding to P-glycoprotein. J Biol Chem. 1987, 262: 2166-2170.PubMed
116.
go back to reference Twentyman PR, Fox NE, White DJ: Cyclosporin A and its analogues as modifiers of adriamycin and vincristine resistance in a multi-drug resistant human lung cancer cell line. Br J Cancer. 1987, 56: 55-57.PubMedCentralPubMed Twentyman PR, Fox NE, White DJ: Cyclosporin A and its analogues as modifiers of adriamycin and vincristine resistance in a multi-drug resistant human lung cancer cell line. Br J Cancer. 1987, 56: 55-57.PubMedCentralPubMed
117.
go back to reference Chauffert B, Martin M, Hammann A, Michel MF, Martin F: Amiodarone-induced enhancement of doxorubicin and 4'-deoxydoxorubicin cytotoxicity to rat colon cancer cells in vitro and in vivo. Cancer Res. 1986, 46: 825-830.PubMed Chauffert B, Martin M, Hammann A, Michel MF, Martin F: Amiodarone-induced enhancement of doxorubicin and 4'-deoxydoxorubicin cytotoxicity to rat colon cancer cells in vitro and in vivo. Cancer Res. 1986, 46: 825-830.PubMed
118.
go back to reference Tsuruo T, Iida H, Kitatani Y, Yokota K, Tsukagoshi S, Sakurai Y: Effects of quinidine and related compounds on cytotoxicity and cellular accumulation of vincristine and adriamycin in drug-resistant tumor cells. Cancer Res. 1984, 44: 4303-4307.PubMed Tsuruo T, Iida H, Kitatani Y, Yokota K, Tsukagoshi S, Sakurai Y: Effects of quinidine and related compounds on cytotoxicity and cellular accumulation of vincristine and adriamycin in drug-resistant tumor cells. Cancer Res. 1984, 44: 4303-4307.PubMed
119.
go back to reference Tsuruo T, Iida H, Tsukagoshi S, Sakurai Y: Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res. 1981, 41: 1967-1972.PubMed Tsuruo T, Iida H, Tsukagoshi S, Sakurai Y: Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res. 1981, 41: 1967-1972.PubMed
120.
go back to reference Murakami N, Sugimoto M, Morita M, Akiyama S, Kobayashi M: Synthesis and evaluation of 4-deacetoxyagosterol A as an MDR-modulator. Bioorg Med Chem Lett. 2000, 10: 2521-2524. 10.1016/S0960-894X(00)00502-3.PubMed Murakami N, Sugimoto M, Morita M, Akiyama S, Kobayashi M: Synthesis and evaluation of 4-deacetoxyagosterol A as an MDR-modulator. Bioorg Med Chem Lett. 2000, 10: 2521-2524. 10.1016/S0960-894X(00)00502-3.PubMed
121.
go back to reference Vezmar M, Georges E: Reversal of MRP-mediated doxorubicin resistance with quinoline-based drugs. Biochem Pharmacol. 2000, 59: 1245-1252. 10.1016/S0006-2952(00)00270-7.PubMed Vezmar M, Georges E: Reversal of MRP-mediated doxorubicin resistance with quinoline-based drugs. Biochem Pharmacol. 2000, 59: 1245-1252. 10.1016/S0006-2952(00)00270-7.PubMed
122.
go back to reference Curtin NJ, Turner DP: Dipyridamole-mediated reversal of multidrug resistance in MRP over-expressing human lung carcinoma cells in vitro. Eur J Cancer. 1999, 35: 1020-1026. 10.1016/S0959-8049(99)00038-6.PubMed Curtin NJ, Turner DP: Dipyridamole-mediated reversal of multidrug resistance in MRP over-expressing human lung carcinoma cells in vitro. Eur J Cancer. 1999, 35: 1020-1026. 10.1016/S0959-8049(99)00038-6.PubMed
123.
go back to reference Terashi K, Oka M, Soda H, Fukuda M, Kawabata S, Nakatomi K, Shiozawa K, Nakamura T, Tsukamoto K, Noguchi Y, Suenaga M, Tei C, Kohno S: Interactions of ofloxacin and erythromycin with the multidrug resistance protein (MRP) in MRP-overexpressing human leukemia cells. Antimicrob Agents Chemother. 2000, 44: 1697-1700. 10.1128/AAC.44.6.1697-1700.2000.PubMedCentralPubMed Terashi K, Oka M, Soda H, Fukuda M, Kawabata S, Nakatomi K, Shiozawa K, Nakamura T, Tsukamoto K, Noguchi Y, Suenaga M, Tei C, Kohno S: Interactions of ofloxacin and erythromycin with the multidrug resistance protein (MRP) in MRP-overexpressing human leukemia cells. Antimicrob Agents Chemother. 2000, 44: 1697-1700. 10.1128/AAC.44.6.1697-1700.2000.PubMedCentralPubMed
124.
go back to reference Payen L, Delugin L, Courtois A, Trinquart Y, Guillouzo A, Fardel O: Reversal of MRP-mediated multidrug resistance in human lung cancer cells by the antiprogestatin drug RU486. Biochem Biophys Res Commun. 1999, 258: 513-518. 10.1006/bbrc.1999.0671.PubMed Payen L, Delugin L, Courtois A, Trinquart Y, Guillouzo A, Fardel O: Reversal of MRP-mediated multidrug resistance in human lung cancer cells by the antiprogestatin drug RU486. Biochem Biophys Res Commun. 1999, 258: 513-518. 10.1006/bbrc.1999.0671.PubMed
125.
go back to reference Nakamura T, Oka M, Aizawa K, Soda H, Fukuda M, Terashi K, Ikeda K, Mizuta Y, Noguchi Y, Kimura Y, Tsuruo T, Kohno S: Direct interaction between a quinoline derivative, MS-209, and multidrug resistance protein (MRP) in human gastric cancer cells. Biochem Biophys Res Commun. 1999, 255: 618-624. 10.1006/bbrc.1999.0245.PubMed Nakamura T, Oka M, Aizawa K, Soda H, Fukuda M, Terashi K, Ikeda K, Mizuta Y, Noguchi Y, Kimura Y, Tsuruo T, Kohno S: Direct interaction between a quinoline derivative, MS-209, and multidrug resistance protein (MRP) in human gastric cancer cells. Biochem Biophys Res Commun. 1999, 255: 618-624. 10.1006/bbrc.1999.0245.PubMed
126.
go back to reference Courtois A, Payen L, Vernhet L, de Vries EG, Guillouzo A, Fardel O: Inhibition of multidrug resistance-associated protein (MRP) activity by rifampicin in human multidrug-resistant lung tumor cells. Cancer Lett. 1999, 139: 97-104. 10.1016/S0304-3835(99)00024-5.PubMed Courtois A, Payen L, Vernhet L, de Vries EG, Guillouzo A, Fardel O: Inhibition of multidrug resistance-associated protein (MRP) activity by rifampicin in human multidrug-resistant lung tumor cells. Cancer Lett. 1999, 139: 97-104. 10.1016/S0304-3835(99)00024-5.PubMed
127.
go back to reference Duffy CP, Elliott CJ, O'Connor RA, Heenan MM, Coyle S, Cleary IM, Kavanagh K, Verhaegen S, O'Loughlin CM, NicAmhlaoibh R, Clynes M: Enhancement of chemotherapeutic drug toxicity to human tumour cells in vitro by a subset of non-steroidal anti-inflammatory drugs (NSAIDs). Eur J Cancer. 1998, 34: 1250-1259. 10.1016/S0959-8049(98)00045-8.PubMed Duffy CP, Elliott CJ, O'Connor RA, Heenan MM, Coyle S, Cleary IM, Kavanagh K, Verhaegen S, O'Loughlin CM, NicAmhlaoibh R, Clynes M: Enhancement of chemotherapeutic drug toxicity to human tumour cells in vitro by a subset of non-steroidal anti-inflammatory drugs (NSAIDs). Eur J Cancer. 1998, 34: 1250-1259. 10.1016/S0959-8049(98)00045-8.PubMed
128.
go back to reference Nagayama S, Chen ZS, Kitazono M, Takebayashi Y, Niwa K, Yamada K, Tani A, Haraguchi M, Sumizawa T, Furukawa T, Aikou T, Akiyama S: Increased sensitivity to vincristine of MDR cells by the leukotriene D4 receptor antagonist, ONO-1078. Cancer Lett. 1998, 130: 175-182. 10.1016/S0304-3835(98)00132-3.PubMed Nagayama S, Chen ZS, Kitazono M, Takebayashi Y, Niwa K, Yamada K, Tani A, Haraguchi M, Sumizawa T, Furukawa T, Aikou T, Akiyama S: Increased sensitivity to vincristine of MDR cells by the leukotriene D4 receptor antagonist, ONO-1078. Cancer Lett. 1998, 130: 175-182. 10.1016/S0304-3835(98)00132-3.PubMed
129.
go back to reference Draper MP, Martell RL, Levy SB: Indomethacin-mediated reversal of multidrug resistance and drug efflux in human and murine cell lines overexpressing MRP, but not P-glycoprotein. Br J Cancer. 1997, 75: 810-815.PubMedCentralPubMed Draper MP, Martell RL, Levy SB: Indomethacin-mediated reversal of multidrug resistance and drug efflux in human and murine cell lines overexpressing MRP, but not P-glycoprotein. Br J Cancer. 1997, 75: 810-815.PubMedCentralPubMed
130.
go back to reference Gollapudi S, Kim CH, Tran BN, Sangha S, Gupta S: Probenecid reverses multidrug resistance in multidrug resistance-associated protein-overexpressing HL60/AR and H69/AR cells but not in P-glycoprotein-overexpressing HL60/Tax and P388/ADR cells. Cancer Chemother Pharmacol. 1997, 40: 150-158. 10.1007/s002800050640.PubMed Gollapudi S, Kim CH, Tran BN, Sangha S, Gupta S: Probenecid reverses multidrug resistance in multidrug resistance-associated protein-overexpressing HL60/AR and H69/AR cells but not in P-glycoprotein-overexpressing HL60/Tax and P388/ADR cells. Cancer Chemother Pharmacol. 1997, 40: 150-158. 10.1007/s002800050640.PubMed
131.
go back to reference Manzano RG, Wright KA, Twentyman PR: Modulation by acrolein and chloroacetaldehyde of multidrug resistance mediated by the multidrug resistance-associated protein (MRP). Clin Cancer Res. 1996, 2: 1321-1326.PubMed Manzano RG, Wright KA, Twentyman PR: Modulation by acrolein and chloroacetaldehyde of multidrug resistance mediated by the multidrug resistance-associated protein (MRP). Clin Cancer Res. 1996, 2: 1321-1326.PubMed
132.
go back to reference Vanhoefer U, Cao S, Minderman H, Toth K, Skenderis BS, Slovak ML, Rustum YM: d,l-buthionine-(S,R)-sulfoximine potentiates in vivo the therapeutic efficacy of doxorubicin against multidrug resistance protein-expressing tumors. Clin Cancer Res. 1996, 2: 1961-1968.PubMed Vanhoefer U, Cao S, Minderman H, Toth K, Skenderis BS, Slovak ML, Rustum YM: d,l-buthionine-(S,R)-sulfoximine potentiates in vivo the therapeutic efficacy of doxorubicin against multidrug resistance protein-expressing tumors. Clin Cancer Res. 1996, 2: 1961-1968.PubMed
133.
go back to reference Vanhoefer U, Cao S, Minderman H, Toth K, Scheper RJ, Slovak ML, Rustum YM: PAK-104P, a pyridine analogue, reverses paclitaxel and doxorubicin resistance in cell lines and nude mice bearing xenografts that overexpress the multidrug resistance protein. Clin Cancer Res. 1996, 2: 369-377.PubMed Vanhoefer U, Cao S, Minderman H, Toth K, Scheper RJ, Slovak ML, Rustum YM: PAK-104P, a pyridine analogue, reverses paclitaxel and doxorubicin resistance in cell lines and nude mice bearing xenografts that overexpress the multidrug resistance protein. Clin Cancer Res. 1996, 2: 369-377.PubMed
134.
go back to reference Gollapudi S, Thadepalli F, Kim CH, Gupta S: Difloxacin reverses multidrug resistance in HL-60/AR cells that overexpress the multidrug resistance-related protein (MRP) gene. Oncol Res. 1995, 7: 213-225.PubMed Gollapudi S, Thadepalli F, Kim CH, Gupta S: Difloxacin reverses multidrug resistance in HL-60/AR cells that overexpress the multidrug resistance-related protein (MRP) gene. Oncol Res. 1995, 7: 213-225.PubMed
135.
go back to reference Gekeler V, Ise W, Sanders KH, Ulrich WR, Beck J: The leukotriene LTD4 receptor antagonist MK571 specifically modulates MRP associated multidrug resistance. Biochem Biophys Res Commun. 1995, 208: 345-352. 10.1006/bbrc.1995.1344.PubMed Gekeler V, Ise W, Sanders KH, Ulrich WR, Beck J: The leukotriene LTD4 receptor antagonist MK571 specifically modulates MRP associated multidrug resistance. Biochem Biophys Res Commun. 1995, 208: 345-352. 10.1006/bbrc.1995.1344.PubMed
136.
go back to reference Zhang S, Yang X, Morris ME: Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol. 2004, 65: 1208-1216. 10.1124/mol.65.5.1208.PubMed Zhang S, Yang X, Morris ME: Flavonoids are inhibitors of breast cancer resistance protein (ABCG2)-mediated transport. Mol Pharmacol. 2004, 65: 1208-1216. 10.1124/mol.65.5.1208.PubMed
137.
go back to reference Imai Y, Tsukahara S, Asada S, Sugimoto Y: Phytoestrogens/Flavonoids Reverse Breast Cancer Resistance Protein/ABCG2-Mediated Multidrug Resistance. Cancer Res. 2004, 64: 4346-4352. 10.1158/0008-5472.CAN-04-0078.PubMed Imai Y, Tsukahara S, Asada S, Sugimoto Y: Phytoestrogens/Flavonoids Reverse Breast Cancer Resistance Protein/ABCG2-Mediated Multidrug Resistance. Cancer Res. 2004, 64: 4346-4352. 10.1158/0008-5472.CAN-04-0078.PubMed
138.
go back to reference Houghton PJ, Germain GS, Harwood FC, Schuetz JD, Stewart CF, Buchdunger E, Traxler P: Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro. Cancer Res. 2004, 64: 2333-2337. 10.1158/0008-5472.CAN-03-3344.PubMed Houghton PJ, Germain GS, Harwood FC, Schuetz JD, Stewart CF, Buchdunger E, Traxler P: Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro. Cancer Res. 2004, 64: 2333-2337. 10.1158/0008-5472.CAN-03-3344.PubMed
139.
go back to reference Sugimoto Y, Tsukahara S, Imai Y, Ueda K, Tsuruo T: Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists. Mol Cancer Ther. 2003, 2: 105-112.PubMed Sugimoto Y, Tsukahara S, Imai Y, Ueda K, Tsuruo T: Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists. Mol Cancer Ther. 2003, 2: 105-112.PubMed
140.
go back to reference Allen JD, van Loevezijn A, Lakhai JM, van der Valk M, van Tellingen O, Reid G, Schellens JH, Koomen GJ, Schinkel AH: Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol Cancer Ther. 2002, 1: 417-425.PubMed Allen JD, van Loevezijn A, Lakhai JM, van der Valk M, van Tellingen O, Reid G, Schellens JH, Koomen GJ, Schinkel AH: Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol Cancer Ther. 2002, 1: 417-425.PubMed
141.
go back to reference de Bruin M, Miyake K, Litman T, Robey R, Bates SE: Reversal of resistance by GF120918 in cell lines expressing the ABC half-transporter, MXR. Cancer Lett. 1999, 146: 117-126. 10.1016/S0304-3835(99)00182-2.PubMed de Bruin M, Miyake K, Litman T, Robey R, Bates SE: Reversal of resistance by GF120918 in cell lines expressing the ABC half-transporter, MXR. Cancer Lett. 1999, 146: 117-126. 10.1016/S0304-3835(99)00182-2.PubMed
142.
go back to reference Rabindran SK, He H, Singh M, Brown E, Collins KI, Annable T, Greenberger LM: Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C. Cancer Res. 1998, 58: 5850-5858.PubMed Rabindran SK, He H, Singh M, Brown E, Collins KI, Annable T, Greenberger LM: Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C. Cancer Res. 1998, 58: 5850-5858.PubMed
143.
go back to reference Sharom FJ, Liu R, Qu Q, Romsicki Y: Exploring the structure and function of the P-glycoprotein multidrug transporter using fluorescence spectroscopic tools. Semin Cell Dev Biol. 2001, 12: 257-265. 10.1006/scdb.2000.0251.PubMed Sharom FJ, Liu R, Qu Q, Romsicki Y: Exploring the structure and function of the P-glycoprotein multidrug transporter using fluorescence spectroscopic tools. Semin Cell Dev Biol. 2001, 12: 257-265. 10.1006/scdb.2000.0251.PubMed
144.
go back to reference Daleke DL: Regulation of transbilayer plasma membrane phospholipid asymmetry. J Lipid Res. 2003, 44: 233-242. 10.1194/jlr.R200019-JLR200.PubMed Daleke DL: Regulation of transbilayer plasma membrane phospholipid asymmetry. J Lipid Res. 2003, 44: 233-242. 10.1194/jlr.R200019-JLR200.PubMed
145.
go back to reference Wolf DC, Horwitz SB: P-glycoprotein transports corticosterone and is photoaffinity-labeled by the steroid. Int J Cancer. 1992, 52: 141-146.PubMed Wolf DC, Horwitz SB: P-glycoprotein transports corticosterone and is photoaffinity-labeled by the steroid. Int J Cancer. 1992, 52: 141-146.PubMed
146.
go back to reference Liu Y, Huang L, Hoffman T, Gosland M, Vore M: MDR1 substrates/modulators protect against beta-estradiol-17beta-D-glucuronide cholestasis in rat liver. Cancer Res. 1996, 56: 4992-4997.PubMed Liu Y, Huang L, Hoffman T, Gosland M, Vore M: MDR1 substrates/modulators protect against beta-estradiol-17beta-D-glucuronide cholestasis in rat liver. Cancer Res. 1996, 56: 4992-4997.PubMed
147.
go back to reference Ernest S, Bello-Reuss E: Secretion of platelet-activating factor is mediated by MDR1 P-glycoprotein in cultured human mesangial cells. J Am Soc Nephrol. 1999, 10: 2306-2313.PubMed Ernest S, Bello-Reuss E: Secretion of platelet-activating factor is mediated by MDR1 P-glycoprotein in cultured human mesangial cells. J Am Soc Nephrol. 1999, 10: 2306-2313.PubMed
148.
go back to reference Liu XD, Liu GQ: P glycoprotein regulated transport of glutamate at blood brain barrier. Acta Pharmacol Sin. 2001, 22: 111-116.PubMed Liu XD, Liu GQ: P glycoprotein regulated transport of glutamate at blood brain barrier. Acta Pharmacol Sin. 2001, 22: 111-116.PubMed
149.
go back to reference King M, Su W, Chang A, Zuckerman A, Pasternak GW: Transport of opioids from the brain to the periphery by P-glycoprotein: peripheral actions of central drugs. Nat Neurosci. 2001, 4: 268-274. 10.1038/85115.PubMed King M, Su W, Chang A, Zuckerman A, Pasternak GW: Transport of opioids from the brain to the periphery by P-glycoprotein: peripheral actions of central drugs. Nat Neurosci. 2001, 4: 268-274. 10.1038/85115.PubMed
150.
go back to reference Vogelgesang S, Cascorbi I, Schroeder E, Pahnke J, Kroemer HK, Siegmund W, Kunert-Keil C, Walker LC, Warzok RW: Deposition of Alzheimer's beta-amyloid is inversely correlated with P-glycoprotein expression in the brains of elderly non-demented humans. Pharmacogenetics. 2002, 12: 535-541. 10.1097/00008571-200210000-00005.PubMed Vogelgesang S, Cascorbi I, Schroeder E, Pahnke J, Kroemer HK, Siegmund W, Kunert-Keil C, Walker LC, Warzok RW: Deposition of Alzheimer's beta-amyloid is inversely correlated with P-glycoprotein expression in the brains of elderly non-demented humans. Pharmacogenetics. 2002, 12: 535-541. 10.1097/00008571-200210000-00005.PubMed
151.
go back to reference Lam FC, Liu R, Lu P, Shapiro AB, Renoir JM, Sharom FJ, Reiner PB: beta-Amyloid efflux mediated by p-glycoprotein. J Neurochem. 2001, 76: 1121-1128. 10.1046/j.1471-4159.2001.00113.x.PubMed Lam FC, Liu R, Lu P, Shapiro AB, Renoir JM, Sharom FJ, Reiner PB: beta-Amyloid efflux mediated by p-glycoprotein. J Neurochem. 2001, 76: 1121-1128. 10.1046/j.1471-4159.2001.00113.x.PubMed
152.
go back to reference Leier I, Jedlitschky G, Buchholz U, Cole SP, Deeley RG, Keppler D: The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates. J Biol Chem. 1994, 269: 27807-27810.PubMed Leier I, Jedlitschky G, Buchholz U, Cole SP, Deeley RG, Keppler D: The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates. J Biol Chem. 1994, 269: 27807-27810.PubMed
153.
go back to reference Jedlitschky G, Leier I, Buchholz U, Barnouin K, Kurz G, Keppler D: Transport of glutathione, glucuronate, and sulfate conjugates by the MRP gene-encoded conjugate export pump. Cancer Res. 1996, 56: 988-994.PubMed Jedlitschky G, Leier I, Buchholz U, Barnouin K, Kurz G, Keppler D: Transport of glutathione, glucuronate, and sulfate conjugates by the MRP gene-encoded conjugate export pump. Cancer Res. 1996, 56: 988-994.PubMed
154.
go back to reference Loe DW, Stewart RK, Massey TE, Deeley RG, Cole SP: ATP-dependent transport of aflatoxin B1 and its glutathione conjugates by the product of the multidrug resistance protein (MRP) gene. Mol Pharmacol. 1997, 51: 1034-1041.PubMed Loe DW, Stewart RK, Massey TE, Deeley RG, Cole SP: ATP-dependent transport of aflatoxin B1 and its glutathione conjugates by the product of the multidrug resistance protein (MRP) gene. Mol Pharmacol. 1997, 51: 1034-1041.PubMed
155.
go back to reference Krishnamurthy P, Ross DD, Nakanishi T, Bailey-Dell K, Zhou S, Mercer KE, Sarkadi B, Sorrentino BP, Schuetz JD: The stem cell marker Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme. J Biol Chem. 2004, 279: 24218-24225. 10.1074/jbc.M313599200.PubMed Krishnamurthy P, Ross DD, Nakanishi T, Bailey-Dell K, Zhou S, Mercer KE, Sarkadi B, Sorrentino BP, Schuetz JD: The stem cell marker Bcrp/ABCG2 enhances hypoxic cell survival through interactions with heme. J Biol Chem. 2004, 279: 24218-24225. 10.1074/jbc.M313599200.PubMed
156.
go back to reference Tsuruoka S, Sugimoto KI, Fujimura A, Imai M, Asano Y, Muto S: P-glycoprotein-mediated drug secretion in mouse proximal tubule perfused in vitro. J Am Soc Nephrol. 2001, 12: 177-181. 10.1159/000051255.PubMed Tsuruoka S, Sugimoto KI, Fujimura A, Imai M, Asano Y, Muto S: P-glycoprotein-mediated drug secretion in mouse proximal tubule perfused in vitro. J Am Soc Nephrol. 2001, 12: 177-181. 10.1159/000051255.PubMed
157.
go back to reference Malingre MM, Beijnen JH, Schellens JH: Oral delivery of taxanes. Invest New Drugs. 2001, 19: 155-162. 10.1023/A:1010635000879.PubMed Malingre MM, Beijnen JH, Schellens JH: Oral delivery of taxanes. Invest New Drugs. 2001, 19: 155-162. 10.1023/A:1010635000879.PubMed
158.
go back to reference Mickley LA, Lee JS, Weng Z, Zhan Z, Alvarez M, Wilson W, Bates SE, Fojo T: Genetic polymorphism in MDR-1: a tool for examining allelic expression in normal cells, unselected and drug-selected cell lines, and human tumors. Blood. 1998, 91: 1749-1756.PubMed Mickley LA, Lee JS, Weng Z, Zhan Z, Alvarez M, Wilson W, Bates SE, Fojo T: Genetic polymorphism in MDR-1: a tool for examining allelic expression in normal cells, unselected and drug-selected cell lines, and human tumors. Blood. 1998, 91: 1749-1756.PubMed
159.
go back to reference Fromm MF: The influence of MDR1 polymorphisms on P-glycoprotein expression and function in humans. Adv Drug Deliv Rev. 2002, 54: 1295-1310. 10.1016/S0169-409X(02)00064-9.PubMed Fromm MF: The influence of MDR1 polymorphisms on P-glycoprotein expression and function in humans. Adv Drug Deliv Rev. 2002, 54: 1295-1310. 10.1016/S0169-409X(02)00064-9.PubMed
160.
go back to reference Brinkmann U, Eichelbaum M: Polymorphisms in the ABC drug transporter gene MDR1. Pharmacogenomics J. 2001, 1: 59-64.PubMed Brinkmann U, Eichelbaum M: Polymorphisms in the ABC drug transporter gene MDR1. Pharmacogenomics J. 2001, 1: 59-64.PubMed
161.
go back to reference Ito S, Ieiri I, Tanabe M, Suzuki A, Higuchi S, Otsubo K: Polymorphism of the ABC transporter genes, MDR1, MRP1 and MRP2/cMOAT, in healthy Japanese subjects. Pharmacogenetics. 2001, 11: 175-184. 10.1097/00008571-200103000-00008.PubMed Ito S, Ieiri I, Tanabe M, Suzuki A, Higuchi S, Otsubo K: Polymorphism of the ABC transporter genes, MDR1, MRP1 and MRP2/cMOAT, in healthy Japanese subjects. Pharmacogenetics. 2001, 11: 175-184. 10.1097/00008571-200103000-00008.PubMed
162.
go back to reference Kerb R, Hoffmeyer S, Brinkmann U: ABC drug transporters: hereditary polymorphisms and pharmacological impact in MDR1, MRP1 and MRP2. Pharmacogenomics. 2001, 2: 51-64. 10.1517/14622416.2.1.51.PubMed Kerb R, Hoffmeyer S, Brinkmann U: ABC drug transporters: hereditary polymorphisms and pharmacological impact in MDR1, MRP1 and MRP2. Pharmacogenomics. 2001, 2: 51-64. 10.1517/14622416.2.1.51.PubMed
163.
go back to reference Moriya Y, Nakamura T, Horinouchi M, Sakaeda T, Tamura T, Aoyama N, Shirakawa T, Gotoh A, Fujimoto S, Matsuo M, Kasuga M, Okumura K: Effects of polymorphisms of MDR1, MRP1, and MRP2 genes on their mRNA expression levels in duodenal enterocytes of healthy Japanese subjects. Biol Pharm Bull. 2002, 25: 1356-1359. 10.1248/bpb.25.1356.PubMed Moriya Y, Nakamura T, Horinouchi M, Sakaeda T, Tamura T, Aoyama N, Shirakawa T, Gotoh A, Fujimoto S, Matsuo M, Kasuga M, Okumura K: Effects of polymorphisms of MDR1, MRP1, and MRP2 genes on their mRNA expression levels in duodenal enterocytes of healthy Japanese subjects. Biol Pharm Bull. 2002, 25: 1356-1359. 10.1248/bpb.25.1356.PubMed
164.
go back to reference Tian R, Koyabu N, Takanaga H, Matsuo H, Ohtani H, Sawada Y: Effects of grapefruit juice and orange juice on the intestinal efflux of P-glycoprotein substrates. Pharm Res. 2002, 19: 802-809. 10.1023/A:1016100715125.PubMed Tian R, Koyabu N, Takanaga H, Matsuo H, Ohtani H, Sawada Y: Effects of grapefruit juice and orange juice on the intestinal efflux of P-glycoprotein substrates. Pharm Res. 2002, 19: 802-809. 10.1023/A:1016100715125.PubMed
165.
go back to reference Kurata Y, Ieiri I, Kimura M, Morita T, Irie S, Urae A, Ohdo S, Ohtani H, Sawada Y, Higuchi S, Otsubo K: Role of human MDR1 gene polymorphism in bioavailability and interaction of digoxin, a substrate of P-glycoprotein. Clin Pharmacol Ther. 2002, 72: 209-219. 10.1067/mcp.2002.126177.PubMed Kurata Y, Ieiri I, Kimura M, Morita T, Irie S, Urae A, Ohdo S, Ohtani H, Sawada Y, Higuchi S, Otsubo K: Role of human MDR1 gene polymorphism in bioavailability and interaction of digoxin, a substrate of P-glycoprotein. Clin Pharmacol Ther. 2002, 72: 209-219. 10.1067/mcp.2002.126177.PubMed
166.
go back to reference Hennessy M, Kelleher D, Spiers JP, Barry M, Kavanagh P, Back D, Mulcahy F, Feely J: St Johns wort increases expression of P-glycoprotein: implications for drug interactions. Br J Clin Pharmacol. 2002, 53: 75-82. 10.1046/j.0306-5251.2001.01516.x.PubMedCentralPubMed Hennessy M, Kelleher D, Spiers JP, Barry M, Kavanagh P, Back D, Mulcahy F, Feely J: St Johns wort increases expression of P-glycoprotein: implications for drug interactions. Br J Clin Pharmacol. 2002, 53: 75-82. 10.1046/j.0306-5251.2001.01516.x.PubMedCentralPubMed
167.
go back to reference Kastin AJ, Fasold MB, Zadina JE: Endomorphins, Met-enkephalin, Tyr-MIF-1, and the P-glycoprotein efflux system. Drug Metab Dispos. 2002, 30: 231-234. 10.1124/dmd.30.3.231.PubMed Kastin AJ, Fasold MB, Zadina JE: Endomorphins, Met-enkephalin, Tyr-MIF-1, and the P-glycoprotein efflux system. Drug Metab Dispos. 2002, 30: 231-234. 10.1124/dmd.30.3.231.PubMed
168.
go back to reference Kawahara M, Sakata A, Miyashita T, Tamai I, Tsuji A: Physiologically based pharmacokinetics of digoxin in mdr1a knockout mice. J Pharm Sci. 1999, 88: 1281-1287. 10.1021/js9901763.PubMed Kawahara M, Sakata A, Miyashita T, Tamai I, Tsuji A: Physiologically based pharmacokinetics of digoxin in mdr1a knockout mice. J Pharm Sci. 1999, 88: 1281-1287. 10.1021/js9901763.PubMed
169.
go back to reference Miyama T, Takanaga H, Matsuo H, Yamano K, Yamamoto K, Iga T, Naito M, Tsuruo T, Ishizuka H, Kawahara Y, Sawada Y: P-glycoprotein-mediated transport of itraconazole across the blood-brain barrier. Antimicrob Agents Chemother. 1998, 42: 1738-1744.PubMedCentralPubMed Miyama T, Takanaga H, Matsuo H, Yamano K, Yamamoto K, Iga T, Naito M, Tsuruo T, Ishizuka H, Kawahara Y, Sawada Y: P-glycoprotein-mediated transport of itraconazole across the blood-brain barrier. Antimicrob Agents Chemother. 1998, 42: 1738-1744.PubMedCentralPubMed
170.
go back to reference Mayer U, Wagenaar E, Dorobek B, Beijnen JH, Borst P, Schinkel AH: Full blockade of intestinal P-glycoprotein and extensive inhibition of blood-brain barrier P-glycoprotein by oral treatment of mice with PSC833. J Clin Invest. 1997, 100: 2430-2436.PubMedCentralPubMed Mayer U, Wagenaar E, Dorobek B, Beijnen JH, Borst P, Schinkel AH: Full blockade of intestinal P-glycoprotein and extensive inhibition of blood-brain barrier P-glycoprotein by oral treatment of mice with PSC833. J Clin Invest. 1997, 100: 2430-2436.PubMedCentralPubMed
171.
go back to reference Schinkel AH, Smit JJ, van Tellingen O, Beijnen JH, Wagenaar E, van Deemter L, Mol CA, van der Valk MA, Robanus-Maandag EC, te Riele HP: Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell. 1994, 77: 491-502. 10.1016/0092-8674(94)90212-7.PubMed Schinkel AH, Smit JJ, van Tellingen O, Beijnen JH, Wagenaar E, van Deemter L, Mol CA, van der Valk MA, Robanus-Maandag EC, te Riele HP: Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell. 1994, 77: 491-502. 10.1016/0092-8674(94)90212-7.PubMed
172.
go back to reference Jonker JW, Smit JW, Brinkhuis RF, Maliepaard M, Beijnen JH, Schellens JH, Schinkel AH: Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J Natl Cancer Inst. 2000, 92: 1651-1656. 10.1093/jnci/92.20.1651.PubMed Jonker JW, Smit JW, Brinkhuis RF, Maliepaard M, Beijnen JH, Schellens JH, Schinkel AH: Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J Natl Cancer Inst. 2000, 92: 1651-1656. 10.1093/jnci/92.20.1651.PubMed
173.
go back to reference Hyde SC, Emsley P, Hartshorn MJ, Mimmack MM, Gileadi U, Pearce SR, Gallagher MP, Gill DR, Hubbard RE, Higgins CF: Structural model of ATP-binding proteins associated with cystic fibrosis, multidrug resistance and bacterial transport. Nature. 1990, 346: 362-365. 10.1038/346362a0.PubMed Hyde SC, Emsley P, Hartshorn MJ, Mimmack MM, Gileadi U, Pearce SR, Gallagher MP, Gill DR, Hubbard RE, Higgins CF: Structural model of ATP-binding proteins associated with cystic fibrosis, multidrug resistance and bacterial transport. Nature. 1990, 346: 362-365. 10.1038/346362a0.PubMed
174.
go back to reference Sonveaux N, Shapiro AB, Goormaghtigh E, Ling V, Ruysschaert JM: Secondary and tertiary structure changes of reconstituted P-glycoprotein. A Fourier transform attenuated total reflection infrared spectroscopy analysis. J Biol Chem. 1996, 271: 24617-24624. 10.1074/jbc.271.40.24617.PubMed Sonveaux N, Shapiro AB, Goormaghtigh E, Ling V, Ruysschaert JM: Secondary and tertiary structure changes of reconstituted P-glycoprotein. A Fourier transform attenuated total reflection infrared spectroscopy analysis. J Biol Chem. 1996, 271: 24617-24624. 10.1074/jbc.271.40.24617.PubMed
175.
go back to reference Rosenberg MF, Velarde G, Ford RC, Martin C, Berridge G, Kerr ID, Callaghan R, Schmidlin A, Wooding C, Linton KJ, Higgins CF: Repacking of the transmembrane domains of P-glycoprotein during the transport ATPase cycle. Embo J. 2001, 20: 5615-5625. 10.1093/emboj/20.20.5615.PubMedCentralPubMed Rosenberg MF, Velarde G, Ford RC, Martin C, Berridge G, Kerr ID, Callaghan R, Schmidlin A, Wooding C, Linton KJ, Higgins CF: Repacking of the transmembrane domains of P-glycoprotein during the transport ATPase cycle. Embo J. 2001, 20: 5615-5625. 10.1093/emboj/20.20.5615.PubMedCentralPubMed
176.
go back to reference Rosenberg MF, Kamis AB, Callaghan R, Higgins CF, Ford RC: Three-dimensional structures of the mammalian multidrug resistance P-glycoprotein demonstrate major conformational changes in the transmembrane domains upon nucleotide binding. J Biol Chem. 2003, 278: 8294-8299. 10.1074/jbc.M211758200.PubMed Rosenberg MF, Kamis AB, Callaghan R, Higgins CF, Ford RC: Three-dimensional structures of the mammalian multidrug resistance P-glycoprotein demonstrate major conformational changes in the transmembrane domains upon nucleotide binding. J Biol Chem. 2003, 278: 8294-8299. 10.1074/jbc.M211758200.PubMed
177.
go back to reference Rosenberg MF, Callaghan R, Ford RC, Higgins CF: Structure of the multidrug resistance P-glycoprotein to 2.5 nm resolution determined by electron microscopy and image analysis. J Biol Chem. 1997, 272: 10685-10694. 10.1074/jbc.272.3.1665.PubMed Rosenberg MF, Callaghan R, Ford RC, Higgins CF: Structure of the multidrug resistance P-glycoprotein to 2.5 nm resolution determined by electron microscopy and image analysis. J Biol Chem. 1997, 272: 10685-10694. 10.1074/jbc.272.3.1665.PubMed
178.
go back to reference Senior AE, Bhagat S: P-glycoprotein shows strong catalytic cooperativity between the two nucleotide sites. Biochemistry. 1998, 37: 831-836. 10.1021/bi9719962.PubMed Senior AE, Bhagat S: P-glycoprotein shows strong catalytic cooperativity between the two nucleotide sites. Biochemistry. 1998, 37: 831-836. 10.1021/bi9719962.PubMed
179.
go back to reference Loo TW, Bartlett MC, Clarke DM: Drug binding in human P-glycoprotein causes conformational changes in both nucleotide-binding domains. J Biol Chem. 2003, 278: 1575-1578. 10.1074/jbc.M211307200.PubMed Loo TW, Bartlett MC, Clarke DM: Drug binding in human P-glycoprotein causes conformational changes in both nucleotide-binding domains. J Biol Chem. 2003, 278: 1575-1578. 10.1074/jbc.M211307200.PubMed
180.
go back to reference Gao M, Cui HR, Loe DW, Grant CE, Almquist KC, Cole SP, Deeley RG: Comparison of the functional characteristics of the nucleotide binding domains of multidrug resistance protein 1. J Biol Chem. 2000, 275: 13098-13108. 10.1074/jbc.275.17.13098.PubMed Gao M, Cui HR, Loe DW, Grant CE, Almquist KC, Cole SP, Deeley RG: Comparison of the functional characteristics of the nucleotide binding domains of multidrug resistance protein 1. J Biol Chem. 2000, 275: 13098-13108. 10.1074/jbc.275.17.13098.PubMed
181.
go back to reference Loo TW, Clarke DM: Identification of residues within the drug-binding domain of the human multidrug resistance P-glycoprotein by cysteine-scanning mutagenesis and reaction with dibromobimane. J Biol Chem. 2000, 275: 39272-39278. 10.1074/jbc.M007741200.PubMed Loo TW, Clarke DM: Identification of residues within the drug-binding domain of the human multidrug resistance P-glycoprotein by cysteine-scanning mutagenesis and reaction with dibromobimane. J Biol Chem. 2000, 275: 39272-39278. 10.1074/jbc.M007741200.PubMed
182.
go back to reference Loo TW, Clarke DM: The transmembrane domains of the human multidrug resistance P-glycoprotein are sufficient to mediate drug binding and trafficking to the cell surface. J Biol Chem. 1999, 274: 24759-24765. 10.1074/jbc.274.35.24759.PubMed Loo TW, Clarke DM: The transmembrane domains of the human multidrug resistance P-glycoprotein are sufficient to mediate drug binding and trafficking to the cell surface. J Biol Chem. 1999, 274: 24759-24765. 10.1074/jbc.274.35.24759.PubMed
183.
go back to reference Consoli U, Priebe W, Ling YH, Mahadevia R, Griffin M, Zhao S, Perez-Soler R, Andreeff M: The novel anthracycline annamycin is not affected by P-glycoprotein-related multidrug resistance: comparison with idarubicin and doxorubicin in HL-60 leukemia cell lines. Blood. 1996, 88: 633-644.PubMed Consoli U, Priebe W, Ling YH, Mahadevia R, Griffin M, Zhao S, Perez-Soler R, Andreeff M: The novel anthracycline annamycin is not affected by P-glycoprotein-related multidrug resistance: comparison with idarubicin and doxorubicin in HL-60 leukemia cell lines. Blood. 1996, 88: 633-644.PubMed
184.
go back to reference Perez-Soler R, Neamati N, Zou Y, Schneider E, Doyle LA, Andreeff M, Priebe W, Ling YH: Annamycin circumvents resistance mediated by the multidrug resistance-associated protein (MRP) in breast MCF-7 and small-cell lung UMCC-1 cancer cell lines selected for resistance to etoposide. Int J Cancer. 1997, 71: 35-41. 10.1002/(SICI)1097-0215(19970328)71:1<35::AID-IJC8>3.0.CO;2-4.PubMed Perez-Soler R, Neamati N, Zou Y, Schneider E, Doyle LA, Andreeff M, Priebe W, Ling YH: Annamycin circumvents resistance mediated by the multidrug resistance-associated protein (MRP) in breast MCF-7 and small-cell lung UMCC-1 cancer cell lines selected for resistance to etoposide. Int J Cancer. 1997, 71: 35-41. 10.1002/(SICI)1097-0215(19970328)71:1<35::AID-IJC8>3.0.CO;2-4.PubMed
185.
go back to reference Mazel M, Clair P, Rousselle C, Vidal P, Scherrmann JM, Mathieu D, Temsamani J: Doxorubicin-peptide conjugates overcome multidrug resistance. Anticancer Drugs. 2001, 12: 107-116. 10.1097/00001813-200102000-00003.PubMed Mazel M, Clair P, Rousselle C, Vidal P, Scherrmann JM, Mathieu D, Temsamani J: Doxorubicin-peptide conjugates overcome multidrug resistance. Anticancer Drugs. 2001, 12: 107-116. 10.1097/00001813-200102000-00003.PubMed
186.
go back to reference Belpomme D, Gauthier S, Pujade-Lauraine E, Facchini T, Goudier MJ, Krakowski I, Netter-Pinon G, Frenay M, Gousset C, Marie FN, Benmiloud M, Sturtz F: Verapamil increases the survival of patients with anthracycline-resistant metastatic breast carcinoma. Ann Oncol. 2000, 11: 1471-1476. 10.1023/A:1026556119020.PubMed Belpomme D, Gauthier S, Pujade-Lauraine E, Facchini T, Goudier MJ, Krakowski I, Netter-Pinon G, Frenay M, Gousset C, Marie FN, Benmiloud M, Sturtz F: Verapamil increases the survival of patients with anthracycline-resistant metastatic breast carcinoma. Ann Oncol. 2000, 11: 1471-1476. 10.1023/A:1026556119020.PubMed
187.
go back to reference Haussermann K, Benz B, Gekeler V, Schumacher K, Eichelbaum M: Effects of verapamil enantiomers and major metabolites on the cytotoxicity of vincristine and daunomycin in human lymphoma cell lines. Eur J Clin Pharmacol. 1991, 40: 53-59. 10.1007/BF00315139.PubMed Haussermann K, Benz B, Gekeler V, Schumacher K, Eichelbaum M: Effects of verapamil enantiomers and major metabolites on the cytotoxicity of vincristine and daunomycin in human lymphoma cell lines. Eur J Clin Pharmacol. 1991, 40: 53-59. 10.1007/BF00315139.PubMed
188.
go back to reference Teodori E, Dei S, Scapecchi S, Gualtieri F: The medicinal chemistry of multidrug resistance (MDR) reversing drugs. Farmaco. 2002, 57: 385-415. 10.1016/S0014-827X(02)01229-6.PubMed Teodori E, Dei S, Scapecchi S, Gualtieri F: The medicinal chemistry of multidrug resistance (MDR) reversing drugs. Farmaco. 2002, 57: 385-415. 10.1016/S0014-827X(02)01229-6.PubMed
189.
go back to reference Toffoli G, Simone F, Corona G, Raschack M, Cappelletto B, Gigante M, Boiocchi M: Structure-activity relationship of verapamil analogs and reversal of multidrug resistance. Biochem Pharmacol. 1995, 50: 1245-1255. 10.1016/0006-2952(95)02003-U.PubMed Toffoli G, Simone F, Corona G, Raschack M, Cappelletto B, Gigante M, Boiocchi M: Structure-activity relationship of verapamil analogs and reversal of multidrug resistance. Biochem Pharmacol. 1995, 50: 1245-1255. 10.1016/0006-2952(95)02003-U.PubMed
190.
go back to reference Slater LM, Sweet P, Stupecky M, Gupta S: Cyclosporin A reverses vincristine and daunorubicin resistance in acute lymphatic leukemia in vitro. J Clin Invest. 1986, 77: 1405-1408.PubMedCentralPubMed Slater LM, Sweet P, Stupecky M, Gupta S: Cyclosporin A reverses vincristine and daunorubicin resistance in acute lymphatic leukemia in vitro. J Clin Invest. 1986, 77: 1405-1408.PubMedCentralPubMed
191.
go back to reference Arceci RJ, Stieglitz K, Bierer BE: Immunosuppressants FK506 and rapamycin function as reversal agents of the multidrug resistance phenotype. Blood. 1992, 80: 1528-1536.PubMed Arceci RJ, Stieglitz K, Bierer BE: Immunosuppressants FK506 and rapamycin function as reversal agents of the multidrug resistance phenotype. Blood. 1992, 80: 1528-1536.PubMed
192.
go back to reference Fracasso PM, Brady MF, Moore DH, Walker JL, Rose PG, Letvak L, Grogan TM, McGuire WP: Phase II study of paclitaxel and valspodar (PSC 833) in refractory ovarian carcinoma: a gynecologic oncology group study. J Clin Oncol. 2001, 19: 2975-2982.PubMed Fracasso PM, Brady MF, Moore DH, Walker JL, Rose PG, Letvak L, Grogan TM, McGuire WP: Phase II study of paclitaxel and valspodar (PSC 833) in refractory ovarian carcinoma: a gynecologic oncology group study. J Clin Oncol. 2001, 19: 2975-2982.PubMed
193.
go back to reference Mistry P, Stewart AJ, Dangerfield W, Okiji S, Liddle C, Bootle D, Plumb JA, Templeton D, Charlton P: In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res. 2001, 61: 749-758.PubMed Mistry P, Stewart AJ, Dangerfield W, Okiji S, Liddle C, Bootle D, Plumb JA, Templeton D, Charlton P: In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res. 2001, 61: 749-758.PubMed
194.
go back to reference Dayan G, Jault JM, Baubichon-Cortay H, Baggetto LG, Renoir JM, Baulieu EE, Gros P, Di Pietro A: Binding of steroid modulators to recombinant cytosolic domain from mouse P-glycoprotein in close proximity to the ATP site. Biochemistry. 1997, 36: 15208-15215. 10.1021/bi9718696.PubMed Dayan G, Jault JM, Baubichon-Cortay H, Baggetto LG, Renoir JM, Baulieu EE, Gros P, Di Pietro A: Binding of steroid modulators to recombinant cytosolic domain from mouse P-glycoprotein in close proximity to the ATP site. Biochemistry. 1997, 36: 15208-15215. 10.1021/bi9718696.PubMed
195.
go back to reference Conseil G, Baubichon-Cortay H, Dayan G, Jault JM, Barron D, Di Pietro A: Flavonoids: a class of modulators with bifunctional interactions at vicinal ATP- and steroid-binding sites on mouse P-glycoprotein. Proc Natl Acad Sci U S A. 1998, 95: 9831-9836. 10.1073/pnas.95.17.9831.PubMedCentralPubMed Conseil G, Baubichon-Cortay H, Dayan G, Jault JM, Barron D, Di Pietro A: Flavonoids: a class of modulators with bifunctional interactions at vicinal ATP- and steroid-binding sites on mouse P-glycoprotein. Proc Natl Acad Sci U S A. 1998, 95: 9831-9836. 10.1073/pnas.95.17.9831.PubMedCentralPubMed
196.
go back to reference Rabindran SK, Ross DD, Doyle LA, Yang W, Greenberger LM: Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein. Cancer Res. 2000, 60: 47-50.PubMed Rabindran SK, Ross DD, Doyle LA, Yang W, Greenberger LM: Fumitremorgin C reverses multidrug resistance in cells transfected with the breast cancer resistance protein. Cancer Res. 2000, 60: 47-50.PubMed
Metadata
Title
ABC transporters as multidrug resistance mechanisms and the development of chemosensitizers for their reversal
Author
Cheol-Hee Choi
Publication date
01-12-2005
Publisher
BioMed Central
Published in
Cancer Cell International / Issue 1/2005
Electronic ISSN: 1475-2867
DOI
https://doi.org/10.1186/1475-2867-5-30

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Cancer Cell International 1/2005 Go to the issue
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Antibody–drug conjugates (ADCs) are novel agents that have shown promise across multiple tumor types. Explore the current landscape of ADCs in breast and lung cancer with our experts, and gain insights into the mechanism of action, key clinical trials data, existing challenges, and future directions.

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