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

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 radiolabele...

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Published in:Molecular imaging and biology 2011-06, Vol.13 (3), p.536
Main Authors: Ying, Yunming, Ghosh, Pradip, Guo, Liwei, Pal, Ashutosh, Mukhapadhyay, Uday, Peng, Zhenghong, Yeh, Hsin Hsien, Bertolini, Susanna, Flores, Leo Garcia, Young, Daniel, Volgin, Andrei, Soghomonyan, Suren, Bornmann, William, Logsdon, Craig, Alauddin, Mian M, Gelovani, Juri G
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container_title Molecular imaging and biology
container_volume 13
creator Ying, Yunming
Ghosh, Pradip
Guo, Liwei
Pal, Ashutosh
Mukhapadhyay, Uday
Peng, Zhenghong
Yeh, Hsin Hsien
Bertolini, Susanna
Flores, Leo Garcia
Young, Daniel
Volgin, Andrei
Soghomonyan, Suren
Bornmann, William
Logsdon, Craig
Alauddin, Mian M
Gelovani, Juri G
description 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'-[^sup 18^F]fluoro-β-d-glucopyranoside (Et-[^sup 18^F]FDL) for noninvasive imaging of pancreatic carcinoma using positron emission tomography and computerized tomography (PET/CT). The novel precursor and radiolabeling methods for synthesis of Et-[^sup 18^F]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-[^sup 18^F]FDL were evaluated using an ex vivo autoradiography and immunohistochemistry in pancreatic tissue sections obtained from mice-bearing orthotopic pancreatic tumor xenografts. Et-[^sup 18^F]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. These results suggest that Et-[^sup 18^F]FDL is a promising agent which should be evaluated for detection of early pancreatic carcinomas by PET/CT imaging.[PUBLICATION ABSTRACT]
doi_str_mv 10.1007/s11307-010-0334-9
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title Synthesis and Ex Vivo Autoradiographic Evaluation of Ethyl-[beta]-d-galactopyranosyl-(1,4')-2'-deoxy-2'-[^sup 18^F]fluoro-[beta]-d-glucopyranoside--A Novel Radioligand for Lactose-Binding Protein: Implications for Early Detection of Pancreatic Carcinomas with PET
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