Top

Published in:

Open Access 01-12-2011 | Review

Transport processes of radiopharmaceuticals and -modulators

Authors: Thomas Efferth, Peter Langguth

Published in: Radiation Oncology | Issue 1/2011

Abstract

Radiotherapy and radiology have been indispensable components in cancer care for many years. The detection limit of small tumor foci as well as the development of radio-resistance and severe side effects towards normal tissues led to the development of strategies to improve radio-diagnostic and -therapeutic approaches by pharmaceuticals. The term "radiopharmaceutical" has been used for drugs labeled with radioactive tracers for therapy or diagnosis. In addition, drugs have been described to sensitize tumor cells to radiotherapy (radiosensitizers) or to protect normal tissues from detrimental effects of radiation (radioprotectors). The present review summarizes recent concepts on the transport of radiopharmaceuticals, radiosensitizers, and radioprotectors in cells and tissues, e.g. by ATP-binding cassette transporters such as P-glycoprotein. Strengths and weaknesses of current strategies to improve transport-based processes are discussed.

Available only for authorised users

Schwochau K: Technetium. Wiley-VCH; 2000.CrossRef

Barth RF, Coderre JA, Graca Vicente MH, Blue TE: Boron neutron capture therapy of cancer: current status and future prospects. Clinical Cancer Research 2005, 11: 3987-4002. 10.1158/1078-0432.CCR-05-0035CrossRefPubMed

Werner S, Schütz C, Grunewald C, Hampel G, Kratz J-V, Nawroth T, Peters T, Langguth P: Enhancement of boronophenylalanine uptake into human hepatoma cells by preloading with L-DOPA and L-tyrosine. , in press.

Efferth T, Fabry U, Osieka R: Apoptosis and resistance to daunorubicin in human leukemic cells. Leukemia 1997, 11: 1180-1186. 10.1038/sj.leu.2400669CrossRefPubMed

Bischoff P, Altmeyer A, Dumont F: Radiosensitising agents for the radiotherapy of cancer: advances in traditional and hypoxia targeted radiosensitisers. Expert Opinion on Therapeutic Patents 2009, 19: 643-662. 10.1517/13543770902824172CrossRefPubMed

Konkimalla VB, Efferth T: Molecular mechanisms and interactions responsible for radio- and chemoresistance of tumors and their modulation by natural products from Ayurveda. In Herbal medicine. A cancer chemopreventive and therapeutic perspective. Edited by: Arora R. Jaypee Brothers Medical Publishers Pvt. Ltd, New Delhi, St. Louis (USA); 2010:513-530.

Shewach DS, Lawrence TS: Antimetabolite radiosensitizers. Journal of Clinical Oncology 2007, 25: 4043-4050. 10.1200/JCO.2007.11.5287CrossRefPubMed

Kelland L: The resurgence of platinum-based cancer chemotherapy. Nature Reviews Cancer 2007, 7: 573-584. 10.1038/nrc2167CrossRefPubMed

Kil WJ, Cerna D, Burgan WE, Beam K, Carter D, Steeg PS, Tofilon PJ, Camphausen K: In vitro and in vivo radiosensitization induced by the DNA methylating agent temozolimide. Clinical Cancer Research 2008, 14: 931-938. 10.1158/1078-0432.CCR-07-1856CrossRefPubMed

10.

Wardman P: Chemical radiosensitizers for use in radiotherapy. In Clinical Oncology. Volume 19. Royal College of Radiologists, Great Britain; 2007:397-417. 10.1016/j.clon.2007.03.010

11.

Seiwert TY, Salama JK, Vokes EE: The concurrent chemoradiation paradigm-general principles. Nature Clinical Practice Oncology 2007, 4: 86-100. 10.1038/ncponc0714CrossRefPubMed

12.

Brown JM: Tumor hypoxia in cancer therapy. Methods in Enzymology 2007, 435: 297-321.PubMed

13.

Overgaard J: Hypoxic radiosensitization: adored and ignored. Journal of Clinical Oncology 2007, 25: 4066-74. 10.1200/JCO.2007.12.7878CrossRefPubMed

14.

Dumont F, Altmeyer A, Bischoff P: Radiosensitising agents for the radiotherapy of cancer: novel molecularly targeted approaches. Expert Opinion on Therapeutic Patents 2009, 19: 775-799. 10.1517/13543770902967666CrossRefPubMed

15.

Efferth T, Fabry U, Glatte P, Osieka R: Expression of apoptosis-related oncoproteins and modulation of apoptosis by caffeine in human leukemic cells. Journal of Cancer Research and Clinical Oncology 1995, 121: 648-56. 10.1007/BF01218522CrossRefPubMed

16.

Tenzer A, Pruschy M: Potentiation of DNA-damage-induced cytotoxicity by G2 checkpoint abrogators. Current Medicinal Chemistry. Anticancer Agents 2003, 3: 35-46. 10.2174/1568011033353533CrossRef

17.

Allison RR, Sibata CH: Photodynamic therapy: mechanism of action and role in the treatment of skin disease. Giornale Italiano Dermatologia e Venereologia 2010, 145: 491-507.

18.

Verhille M, Couleaud P, Vanderesse R, Brault D, Barberi-Heyob M, Frochot C: Modulation of photosensitization processes for an improved targeted photodynamic therapy. Current Medicinal Chemistry 2010, 17: 3925-3943. 10.2174/092986710793205453CrossRefPubMed

19.

Hariharan M, Karunakaran SC, Ramaiah D, Schulz I, Epe B: Photoinduced DNA damage efficiency and cytotoxicity of novel viologen linked pyrene conjugates. Chemical Communications (Cambridge, England) 2010, 46: 2064-2066. 10.1039/b924943eCrossRef

20.

Efferth T, Fabry U, Osieka R: Induction of apoptosis, depletion of glutathione, and DNA damage by extracorporeal photochemotherapy and psoralen with exposure to UV light in vitro. Anticancer Research 2001, 21: 2777-2783.PubMed

21.

Shephard SE, Langguth P, Panizzon RG: Pharmacokinetic behaviour of sublingually administered 8-methoxypsoralen for PUVA therapy. Photodermatology, Photoimmunology and Photomedicine 2001, 17: 11-21. 10.1034/j.1600-0781.2001.017001011.xCrossRefPubMed

22.

Pothiawala SZ, Baldwin BT, Cherpelis BS, Lien MH, Fenske NA: The role of phototherapy in cutaneous T-cell lymphoma. Journal of Drugs in Dermatology 2010, 9: 764-772.PubMed

23.

Ishikawa T, Nakagawa H, Hagiya Y, Nonoguchi N, Miyatake S, Kuroiwa T: Key role of human ABC transporter ABCG2 in photodynamic therapy and photodynamic diagnosis. Advances in Pharmacological Sciences 2010, 2010: 587306.PubMedCentralCrossRefPubMed

24.

Usuda J, Tsunoda Y, Ichinose S, Ishizumi T, Ohtani K, Maehara S, Ono S, Tsutsui H, Ohira T, Okunaka T, Furukawa K, Sugimoto Y, Kato H, Ikeda N: Breast cancer resistant protein (BCRP) is a molecular determinant of the outcome of photodynamic therapy (PDT) for centrally located early lung cancer. Lung Cancer 2010, 67: 198-204. 10.1016/j.lungcan.2009.04.002CrossRefPubMed

25.

Gudkov AV, Komarova EA: Radioprotection: smart games with death. The Journal of Clinical Investigation 2010, 120: 2270-2273. 10.1172/JCI43794PubMedCentralCrossRefPubMed

26.

Girdhani S, Bhosle SM, Thulsidas SA, Kumar A, Mishra KP: Potential of radiosensitizing agents in cancer chemo-radiotherapy. Journal of Cancer Research and Therapeutics 2005, 1: 129-31. 10.4103/0973-1482.19585CrossRefPubMed

27.

Dziegielewski J, Goetz W, Baulch JE: Heavy ions, radioprotectors and genomic instability: implications for human space exploration. Radiation and Environmental Biophysics 2010, 49: 303-316. 10.1007/s00411-009-0261-9CrossRefPubMed

28.

Burdelya LG, Krivokrysenko VI, Tallant TC, Strom E, Gleiberman AS, Gupta D, Kurnasov OV, Fort FL, Osterman AL, Didonato JA, Feinstein E, Gudkov AV: An agonist of toll-like receptor 5 has radioprotective activity in mouse and primate models. Science 2008, 320: 226-230. 10.1126/science.1154986PubMedCentralCrossRefPubMed

29.

Johnson SM, Torrice CD, Bell JF, Monahan KB, Jiang Q, Wang Y, Ramsey MR, Jin J, Wong KK, Su L, Zhou D, Sharpless NE: Mitigation of hematologic radiation toxicity in mice through pharmacological quiescence induced by CDK4/6 inhibition. The Journal of Clinical Investigation 2010, 120: 2528-2536. 10.1172/JCI41402PubMedCentralCrossRefPubMed

30.

Efferth T: Molekulare Pharmakologie und Toxikologie. Springer Verlag, Heidelberg; 2006.

31.

Efferth T: The human ATP-binding cassette transporter genes: from the bench to the bedside. Current Molecular Medicine 2001, 1: 45-65. 10.2174/1566524013364194CrossRefPubMed

32.

Gillet JP, Efferth T, Steinbach D, Hamels J, de Longueville F, Bertholet V, Remacle J: Microarray-based detection of multidrug resistance in human tumor cells by expression profiling of ATP-binding cassette transporter genes. Cancer Research 2004, 64: 8987-8993. 10.1158/0008-5472.CAN-04-1978CrossRefPubMed

33.

Gillet JP, Efferth T, Remacle J: Chemotherapy-induced resistance by ATP-binding cassette transporter genes. Biochimica et Biophysica Acta 2007, 1775: 237-262.PubMed

34.

Efferth T, Gillet JP, Sauerbrey A, Zintl F, Bertholet V, de Longueville F, Remacle J, Steinbach D: Expression profiling of ATP-binding cassette transporters in childhood T-cell acute lymphoblastic leukemia. Molecular Cancer Therapeutics 2006, 5: 1986-1994. 10.1158/1535-7163.MCT-06-0086CrossRefPubMed

35.

Steinbach D, Gillet JP, Sauerbrey A, Gruhn B, Dawczynski K, Bertholet V, de Longueville F, Zintl F, Remacle J, Efferth T: ABCA3 as a possible cause of drug resistance in childhood acute myeloid leukemia. Clinical Cancer Research 2006, 12: 4357-4363. 10.1158/1078-0432.CCR-05-2587CrossRefPubMed

36.

Mahringer A, Karamustafa S, Klotz D, Kahl S, Konkimalla VB, Wang Y, Wang J, Liu HY, Boechzelt H, Hao X, Bauer R, Fricker G, Efferth T: Inhibition of P-glycoprotein at the blood-brain barrier by phytochemicals derived from traditional Chinese medicine. Cancer Genomics and Proteomics 2010, 7: 191-205.PubMed

37.

Zhang EY, Knipp GT, Ekins S, Swaan PW: Structural biology and function of solute transporters: implications for identifying and designing substrates. Drug Metabolism Reviews 2002, 34: 709-750. 10.1081/DMR-120015692CrossRefPubMed

38.

Hagenbuch B, Meier PJ: Organic anion transporting polypeptides of the OATP/SLC21 family: phylogenetic classification as OATP/SLCO superfamily, new nomenclature and molecular/functional properties. Pfluegers Archiv: European Journal of Physiology 2004, 447: 653-665. 10.1007/s00424-003-1168-yCrossRefPubMed

39.

Hagenbuch B: Drug uptake systems in liver and kidney: a historic perspective. Clinical Pharmacology and Therapeutics 2010, 87: 39-47. 10.1038/clpt.2009.235PubMedCentralCrossRefPubMed

40.

Efferth T, Benakis A, Romero MR, Tomicic M, Rauh R, Steinbach D, Häfer R, Stamminger T, Oesch F, Kaina B, Marschall M: Enhancement of cytotoxicity of artemisinins toward cancer cells by ferrous iron. Free Radical Biology and Medicine 2004, 37: 998-1009. 10.1016/j.freeradbiomed.2004.06.023CrossRefPubMed

41.

Kelter G, Steinbach D, Konkimalla VB, Tahara T, Taketani S, Fiebig HH, Efferth T: Role of transferrin receptor and the ABC transporters ABCB6 and ABCB7 for resistance and differentiation of tumor cells towards artesunate. PLoS One 2007, 2: e798. 10.1371/journal.pone.0000798PubMedCentralCrossRefPubMed

42.

Warburg O: On the origin of cancer cells. Science 1956, 123: 309-314. 10.1126/science.123.3191.309CrossRefPubMed

43.

Hühn E, Buchholz HG, Shazly G, Maus S, Thews O, Bausbacher N, Rösch F, Schreckenberger M, Langguth P: Predicting the in vivo release from a liposomal formulation by IVIVC and non-invasive positron emission tomography imaging. European Journal of Pharmaceutical Sciences 2010, 41: 71-77. 10.1016/j.ejps.2010.05.020CrossRefPubMed

44.

Couturier O, Luxen A, Chatal J-F, Vuillez J-P, Rigo P, Hustinx R: Fluorinated tracers for imaging cancer with positron emission tomography. European Journal of Nuclear Medicine and Molecular Imaging 2004, 31: 1182-1206.CrossRefPubMed

45.

Carrasco N: Iodide transport in the thyroid gland. Biochimica et Biophysica Acta 1993, 1154: 65-82.CrossRefPubMed

46.

Tazebay U, Wapnir I, Levy O, Tazebay UH, Wapnir IL, Levy O, Dohan O, Zuckier LS, Zhao QH, Deng HF, Amenta PS, Fineberg S, Pestell RG, Carrasco N: The mammary gland iodide transporter is expressed during lactation and in breast cancer. Nature Medicine 2000, 6: 871-878. 10.1038/78630CrossRefPubMed

47.

Ballinger JR, Hua HA, Berry BW, Firby P, Boxen I: 99mTc-sestamibi as an agent for imaging P-glycoprotein-mediated multi-drug resistance: in vitro and in vivo studies in a rat breast tumour cell line and its doxorubicin-resistant variant. Nuclear Medicine Communications 1995, 16: 253-257. 10.1097/00006231-199504000-00156CrossRefPubMed

48.

Cordobes MD, Starzec A, Delmon-Moingeon L, Blanchot C, Kouyoumdjian JC, Prévost G, Caglar M, Moretti JL: Technetium-99m-sestamibi uptake by human benign and malignant breast tumor cells: correlation with mdr gene expression. Journal of Nuclear Medicine 1996, 37: 286-289.PubMed

49.

Chen WS, Luker KE, Dahlheimer JL, Pica CM, Luker GD, Piwnica-Worms D: Effects of MDR1 and MDR3 P-glycoproteins, MRP1 and BCRP/MXR/ABCP on transport of Tc-99m-tetrofosmin. Biochemical Pharmacology 2000, 60: 413-426. 10.1016/S0006-2952(00)00341-5CrossRefPubMed

50.

Vecchio SD, Ciarmiello A, Potena MI, Carriero MV, Mainolfi C, Botti G, Thomas R, Cerra M, D'Aiuto G, Tsuruo T, Salvatore M: In vivo detection of multidrug resistance (MDR1) phenotype by technetium-99m-sestamibi scan in untreated breast cancer patients. European Journal of Nuclear Medicine 1997, 24: 150-159. 10.1007/BF02439547CrossRefPubMed

51.

Del Vecchio S, Ciarmiello A, Pace L, Potena MI, Carriero MV, Mainolfi C, Thomas R, D'Aiuto G, Tsuruo T, Salvatore M: Fractional retention of technetium-99m-sestamibi as an index of P-glycoprotein expression in untreated breast cancer patients. Journal of Nuclear Medicine 1997, 38: 1348-1351.PubMed

52.

Kostakoglu L, Elahi N, Kïratlï P, Ruacan S, Sayek I, Baltalï E, Sungur A, Hayran M, Bekdik CF: Clinical validation of the influence of P-glycoprotein on technetium-99m-sestamibi uptake in malignant tumors. Journal of Nuclear Medicine 1994, 38: 1003-1008.

53.

Fukumoto M, Yoshida D, Hayase N, Kurohara A, Akagi N, Yoshida S: Scintigraphic prediction of resistance to radiation and chemotherapy in patients with lung carcinoma: technetium 99m-tetrofosmin and thallium-201 dual single photon emission computed tomography study. Cancer 1999, 86: 1470-1479. 10.1002/(SICI)1097-0142(19991015)86:8<1470::AID-CNCR13>3.0.CO;2-SCrossRefPubMed

54.

Hendrikse NH, Franssen EJ, van der Graaf WT, Meijer C, Piers DA, Vaalburg W, de Vries EG: 99mTc-sestamibi is a substrate for P-glycoprotein and the multidrug resistance-associated protein. British Journal of Cancer 1998, 77: 353-358. 10.1038/bjc.1998.57PubMedCentralCrossRefPubMed

55.

Kao CH, Ho YJ, Shen YY, Lee JK: Evaluation of chemotherapy response in patients with small cell lung cancer using Technetium-99m-tetrofosmin. Anticancer Research 1999, 19: 2311-5.PubMed

56.

Kao A, Shuin SC, Hsu NY, Sun SS, Lee CC, Lin CC: Technetium-99m methoxyisobuthylisonitrile chest imaging for small-cell lung cancer. Annals of Oncology 2001, 12: 1561-1566. 10.1023/A:1013133801173CrossRefPubMed

57.

Liang JA, Shiau YC, Yang SN, Lin FJ, Lin CC, Kao A, Lee CC: Using technetium-99m-tetrofosmin scan to predict chemotherapy response of malignant lymphomas, compared with P-glycoprotein and multidrug resistance related protein expression. Oncology Reports 2002, 9: 307-12.PubMed

58.

Thacker J, Stretch A, Stephens MA: The induction of thioguanine-resistant mutants of Chinese hamster cells by gamma-rays. Mutatation Research 1977, 42: 313-326.CrossRef

59.

Osmak M, Perovic S: Multiple fractions of gamma rays induced resistance to cis-dichloro-diammineplatinum (II) and methotrexate in human HeLa cells. International Journal of Radiation Oncology Biology and Physics 1989, 16: 1537-1541. 10.1016/0360-3016(89)90959-0CrossRef

60.

Hill BT, Deuchars K, Hosking LK, Ling V, Whelan RD: Overexpression of P-glycoprotein in mammalian tumor cell lines after fractionated X irradiation in vitro. Journal of the National Cancer Institute 1990, 82: 607-612. 10.1093/jnci/82.7.607CrossRefPubMed

61.

McClean S, Hill BT: Evidence of post-translational regulation of P-glycoprotein associated with the expression of a distinctive multiple drug-resistant phenotype in Chinese hamster ovary cells. European Journal of Cancer 1993, 29A: 2243-2248.CrossRefPubMed

62.

Mattern J, Efferth T, Volm M: Overexpression of P-glycoprotein in human lung carcinoma xenografts after fractionated irradiation in vivo. Radiation Research 1991, 127: 335-338. 10.2307/3577949CrossRefPubMed

63.

Stammler G, Pommerenke EW, Masanek U, Mattern J, Volm M: Messenger RNA expression of resistance factors in human tumor cell lines after single exposure to radiation. Journal of Experimental Therapeutics and Oncology 1996, 1: 39-48.PubMed

64.

Harvie RM, Davey MW, Davey RA: Increased MRP expression is associated with resistance to radiation, anthracyclines and etoposide in cells treated with fractionated gamma-radiation. International Journal of Cancer 1997, 73: 164-167. 10.1002/(SICI)1097-0215(19970926)73:1<164::AID-IJC25>3.0.CO;2-FCrossRef

65.

Bottke D, Koychev D, Busse A, Heufelder K, Wiegel T, Thiel E, Hinkelbein W, Keilholz U: Fractionated irradiation can induce functionally relevant multidrug resistance gene and protein expression in human tumor cell lines. Radiation Research 2008, 170: 41-48. 10.1667/RR0986.1CrossRefPubMed

66.

Denko NC: Hypoxia, HIF1 and glucose metabolism in the solid tumour. Nature Reviews Cancer 2008, 8: 705-713. 10.1038/nrc2468CrossRefPubMed

67.

Nakae T, Uto Y, Tanaka M, Shibata H, Nakata E, Tominaga M, Maezawa H, Hashimoto T, Kirk KL, Nagasawa H, Hori H: Design, synthesis, and radiosensitizing activities of sugar-hybrid hypoxic cell radiosensitizers. Bioorganic and Medicinal Chemistry 2008, 16: 675-682. 10.1016/j.bmc.2007.10.035CrossRefPubMed

68.

Anderson P, Aguilera D, Pearson M, Woo S: Outpatient chemotherapy plus radiotherapy in sarcomas: improving cancer control with radiosensitizing agents. Cancer Control 2008, 15: 38-46.PubMed

69.

Maity A, Tuttle SW: 2-Deoxyglucose and radiosensitization: teaching an old DOG new tricks? Cancer Biology and Therapy 2006, 5: 824-826. 10.4161/cbt.5.7.3024CrossRefPubMed

70.

Dwarakanath BS: Cytotoxicity, radiosensitization, and chemosensitization of tumor cells by 2-deoxy-D-glucose In vitro. Journal of Cancer Research and Therapeutics 2009, 5: 27-31. 10.4103/0973-1482.55137CrossRef

71.

El-Khoury V, Breuzard G, Fourré N, Dufer J: The histone deacetylase inhibitor trichostatin A downregulates human MDR1 (ABCB1) gene expression by a transcription-dependent mechanism in a drug-resistant small cell lung carcinoma cell line model. British Journal of Cancer 2007, 97: 562-573. 10.1038/sj.bjc.6603914PubMedCentralCrossRefPubMed

72.

McCollum AK, TenEyck CJ, Stensgard B, Morlan BW, Ballman KV, Jenkins RB, Toft DO, Erlichman C: P-Glycoprotein-mediated resistance to Hsp90-directed therapy is eclipsed by the heat shock response. Cancer Research 2008, 68: 7419-7427. 10.1158/0008-5472.CAN-07-5175PubMedCentralCrossRefPubMed

73.

Pham AN, Wang J, Fang J, Gao X, Zhang Y, Blower PE, Sadée W, Huang Y: Pharmacogenomics approach reveals MRP1 (ABCC1)-mediated resistance to geldanamycins. Pharmaceutical Research 2009, 26: 936-945. 10.1007/s11095-008-9796-8CrossRefPubMed

74.

García MG, Alaniz LD, Cordo Russo RI, Alvarez E, Hajos SE: PI3K/Akt inhibition modulates multidrug resistance and activates NF-kappaB in murine lymphoma cell lines. Leukemia Research 2009, 33: 288-296. 10.1016/j.leukres.2008.06.010CrossRefPubMed

75.

Tazzari PL, Cappellini A, Ricci F, Evangelisti C, Papa V, Grafone T, Martinelli G, Conte R, Cocco L, McCubrey JA, Martelli AM: Multidrug resistance-associated protein 1 expression is under the control of the phosphoinositide 3 kinase/Akt signal transduction network in human acute myelogenous leukemia blasts. Leukemia 2007, 21: 427-438. 10.1038/sj.leu.2404523CrossRefPubMed

76.

Furtado LM, Somwar R, Sweeney G, Niu W, Klip A: Activation of the glucose transporter GLUT4 by insulin. Biochemistry and Cell Biology 2002, 80: 569-578. 10.1139/o02-156CrossRefPubMed

77.

Cantuaria G, Fagotti A, Ferrandina G, Magalhaes A, Nadji M, Angioli R, Penalver M, Mancuso S, Scambia G: GLUT-1 expression in ovarian carcinoma: association with survival and response to chemotherapy. Cancer 2001, 92: 1144-1150. 10.1002/1097-0142(20010901)92:5<1144::AID-CNCR1432>3.0.CO;2-TCrossRefPubMed

78.

Alvarez AI, Real R, Perez M, Mendoza G, Prieto JG, Merino G: Modulation of the activity of ABC transporters (P-glycoprotein, MRP2, BCRP) by flavonoids and drug response. Journal of Pharmaceutical Sciences 2010, 22: 598-617.

79.

Choi JS, Choi BC, Kang KW: Effect of resveratrol on the pharmacokinetics of oral and intravenous nicardipine in rats: possible role of P-glycoprotein inhibition by resveratrol. Pharmazie 2009, 64: 49-52.PubMed

80.

Baumert C, Hilgeroth A: Recent advances in the development of P-gp inhibitors. Anticancer Agents in Medicinal Chemistry 2009, 9: 415-436.CrossRef

81.

Tiwar AK, Sodani K, Dai CL, Ashby CR Jr, Chen ZS: Revisiting the ABCs of Multidrug Resistance in Cancer Chemotherapy. Current Pharmaceutical Biotechnology 2010, in press.

82.

Molnár J, Engi H, Hohmann J, Molnár P, Deli J, Wesolowska O, Michalak K, Wang Q: Reversal of multidrug resitance by natural substances from plants. Current Topics in Medicinal Chemistry 2010, 10: 1757-1768. 10.2174/156802610792928103CrossRefPubMed

83.

Eichhorn T, Efferth T: P-glycoprotein and its Inhibition in Tumors by Phytochemicals derived from Traditional Chinese Medicine. Journal of Ethnopharmacology 2011, in press.

84.

Versantvoort CH, Broxterman HJ, Lankelma J, Feller N, Pinedo HM: Competitive inhibition by genistein and ATP dependence of daunorubicin transport in intact MRP overexpressing human small cell lung cancer cells. Biochemical Pharmacology 1994, 48: 1129-1136. 10.1016/0006-2952(94)90149-XCrossRefPubMed

85.

Nabekura T, Yamaki T, Ueno K, Kitagawa S: Inhibition of P-glycoprotein and multidrug resistance protein 1 by dietary phytochemicals. Cancer Chemotherapy and Pharmacology 2008, 62: 867-873. 10.1007/s00280-007-0676-4CrossRefPubMed

86.

Wesolowska O, Wisniewski J, Sroda K, Krawczenko A, Bielawska-Pohl A, Paprocka M, Dus D, Michalak K: 8-Prenylnaringenin is an inhibitor of multidrug resistance-associated transporters, P-glycoprotein and MRP1. European Journal of Pharmacology 2010, 644: 32-40. 10.1016/j.ejphar.2010.06.069CrossRefPubMed

87.

Ahmed-Belkacem A, Pozza A, Macalou S, Pérez-Victoria JM, Boumendjel A, Di Pietro A: Inhibitors of cancer cell multidrug resistance mediated by breast cancer resistance protein (BCRP/ABCG2). Anticancer Drugs 2006, 17: 239-243. 10.1097/00001813-200603000-00001CrossRefPubMed

88.

Boumendjel A, McLeer-Florin A, Champelovier P, Allegro D, Muhammad D, Souard F, Derouazi M, Peyrot V, Toussaint B, Boutonnat J: A novel chalcone derivative which acts as a microtubule depolymerising agent and an inhibitor of P-gp and BCRP in in-vitro and in-vivo glioblastoma models. BMC Cancer 2009, 9: 242. 10.1186/1471-2407-9-242PubMedCentralCrossRefPubMed

89.

Farabegoli F, Papi A, Bartolini G, Ostan R, Orlandi M: (-)-Epigallocatechin-3-gallate downregulates Pg-P and BCRP in a tamoxifen resistant MCF-7 cell line. Phytomedicine 2010, 17: 356-362. 10.1016/j.phymed.2010.01.001CrossRefPubMed

90.

Mitchell JL, Judd GG, Diveley RR Jr, Choe CY, Leyser A: Involvement of the polyamine transport system in cellular uptake of the radioprotectants WR-1065 and WR-33278. In Carcinogenesis. Volume 16. Lond.; 1995:3063-3068. 10.1093/carcin/16.12.3063

91.

Newton GL, Aguilera JA, Kim T, Ward JF, Fahey RC: Transport of aminothiol radioprotectors into mammalian cells: passive diffusion versus mediated uptake. Radiation Research 1996, 146: 206-215. 10.2307/3579592CrossRefPubMed

92.

Quiñones HI, List AF, Gerner EW: Selective Exclusion by the Polyamine Transporter as a Mechanism for Differential Radioprotection of Amifostine Derivatives. Clinical Cancer Research 2008, 8: 1295-1300.

93.

Lamperti A, Ziskin MC, Bergey E, Gorlowski J, Sodicoff M: Transdermal absorption of radioprotectors in the rat using permeation-enhancing vehicles. Radiation Research 1990, 124: 194-200. 10.2307/3577866CrossRefPubMed

94.

Maier P, Fleckenstein K, Li L, Laufs S, Zeller WJ, Baum C, Fruehauf S, Herskind C, Wenz F: Overexpression of MDR1 using a retroviral vector differentially regulates genes involved in detoxification and apoptosis and confers radioprotection. Radiation Research 2006, 166: 463-473. 10.1667/RR0550.1CrossRefPubMed

95.

Hilgendorf C, Spahn-Langguth H, Rhedin M, Regårdh CG, Löwenadler B, Langguth P: Selective downregulation of the MDR1 gene product in Caco-2 cells by stable transfection to prove its relevance in secretory drug transport. Molecular Pharmaceutics 2005, 2: 64-73. 10.1021/mp049931yCrossRefPubMed

96.

Lebrun F, Benderitter M, Berroud A, Voisin P, Griffiths NM: Potential role of the membrane in the development of intestinal cellular damage after whole-body gamma irradiation of the rat. Canadian Journal of Physiology and Pharmacology 2002, 80: 686-693. 10.1139/y02-091CrossRefPubMed

97.

Kaempf-Rotzolla DE, Traberc MG, Arai H: Vitamin E and transfer proteins. Current Opinion in Lipidology 2003, 14: 249-254. 10.1097/00041433-200306000-00004CrossRef

98.

Lemaire-Ewing S, Desrumaux C, Neel D, Lagrost L: Vitamin E transport, membrane incorporation and cell metabolism: Is a-tocopherol in lipid rafts an oar in the lifeboat? Molecular Nutrition and Food Research 2010, 54: 631-640. 10.1002/mnfr.200900445CrossRefPubMed

Title: Transport processes of radiopharmaceuticals and -modulators
Authors: Thomas Efferth
Peter Langguth
Publication date: 01-12-2011
Publisher: BioMed Central
Published in: Radiation Oncology / Issue 1/2011
Electronic ISSN: 1748-717X
DOI: https://doi.org/10.1186/1748-717X-6-59

At a glance: The STEP trials

Springer Medicine

Transport processes of radiopharmaceuticals and -modulators

Abstract

At a glance: The STEP trials

Springer Medicine

Abstract

Please log in to get access to this content

Other articles of this Issue 1/2011

Recurrence patterns of locally advanced head and neck squamous cell carcinoma after 3D conformal (chemo)-radiotherapy

Dysphagia in head and neck cancer patients following intensity modulated radiotherapy (IMRT)

Antiangiogenic agents in the treatment of recurrent or newly diagnosed glioblastoma: Analysis of single-agent and combined modality approaches

Comparison of outcomes in patients with stage III versus limited stage IV non-small cell lung cancer

Survival Analysis of F98 Glioma Rat Cells Following Minibeam or Broad-Beam Synchrotron Radiation Therapy

Preliminary comp arison of helical tomotherapy and mixed beams of unmodulated electrons and intensity modulated radiation therapy for treating superficial cancers of the parotid gland and nasal cavity