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01-06-2011 | Research Article

Synthesis and Ex Vivo Autoradiographic Evaluation of Ethyl-β-d-galactopyranosyl-(1,4′)-2′-deoxy-2′-[¹⁸F]fluoro-β-d-glucopyranoside—A Novel Radioligand for Lactose-Binding Protein: Implications for Early Detection of Pancreatic Carcinomas with PET

Authors: Yunming Ying, Pradip Ghosh, Liwei Guo, Ashutosh Pal, Uday Mukhapadhyay, Zhenghong Peng, Hsin Hsien Yeh, Susanna Bertolini, Leo Garcia Flores, Daniel Young, Andrei Volgin, Suren Soghomonyan, William Bornmann, Craig Logsdon, Mian M. Alauddin, Juri G. Gelovani

Published in: Molecular Imaging and Biology | Issue 3/2011

Abstract

Introduction

Previous studies demonstrated that the lactose-binding protein (hepatocellular carcinoma–intestine–pancreas and pancreatitis-associated proteins (HIP/PAP)) is upregulated >130 times in peritumoral pancreatic tissue as compared to normal pancreatic tissue. Therefore, we developed a new radiolabeled ligand of HIP/PAP, the ethyl-β-d-galactopyranosyl-(1,4′)-2′-deoxy-2′-[¹⁸F]fluoro-β-d-glucopyranoside (Et-[¹⁸F]FDL) for noninvasive imaging of pancreatic carcinoma using positron emission tomography and computerized tomography (PET/CT).

Methods

The novel precursor and radiolabeling methods for synthesis of Et-[¹⁸F]FDL produced no isomers; the average decay-corrected radiochemical yield was 68%, radiochemical purity >99%, and specific activity >74 GBq/µmol. The radioligand properties of Et-[¹⁸F]FDL were evaluated using an ex vivo autoradiography and immunohistochemistry in pancreatic tissue sections obtained from mice-bearing orthotopic pancreatic tumor xenografts.

Results and Discussion

Et-[¹⁸F]FDL binding to peritumoral pancreatic tissue sections strongly correlated with HIP/PAP expression (r = 0.81) and could be completely blocked by treatment with 1 mM lactose.

Conclusion

These results suggest that Et-[¹⁸F]FDL is a promising agent which should be evaluated for detection of early pancreatic carcinomas by PET/CT imaging.

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Title: Synthesis and Ex Vivo Autoradiographic Evaluation of Ethyl-β-d-galactopyranosyl-(1,4′)-2′-deoxy-2′-[18F]fluoro-β-d-glucopyranoside—A Novel Radioligand for Lactose-Binding Protein: Implications for Early Detection of Pancreatic Carcinomas with PET
Authors: Yunming Ying
Pradip Ghosh
Liwei Guo
Ashutosh Pal
Uday Mukhapadhyay
Zhenghong Peng
Hsin Hsien Yeh
Susanna Bertolini
Leo Garcia Flores
Daniel Young
Andrei Volgin
Suren Soghomonyan
William Bornmann
Craig Logsdon
Mian M. Alauddin
Juri G. Gelovani
Publication date: 01-06-2011
Publisher: Springer-Verlag
Published in: Molecular Imaging and Biology / Issue 3/2011
Print ISSN: 1536-1632
Electronic ISSN: 1860-2002
DOI: https://doi.org/10.1007/s11307-010-0334-9

At a glance: The STEP trials

Springer Medicine

Synthesis and Ex Vivo Autoradiographic Evaluation of Ethyl-β-d-galactopyranosyl-(1,4′)-2′-deoxy-2′-[¹⁸F]fluoro-β-d-glucopyranoside—A Novel Radioligand for Lactose-Binding Protein: Implications for Early Detection of Pancreatic Carcinomas with PET

Abstract

Introduction

Methods

Results and Discussion

Conclusion

At a glance: The STEP trials

Springer Medicine

Abstract

Introduction

Methods

Results and Discussion

Conclusion

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