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Synthesis and Ex Vivo Autoradiographic Evaluation of Ethyl-β-D: -galactopyranosyl-(1,4')-2'-deoxy-2'-[(18)F]fluoro-β-D: -glucopyranoside-A Novel Radioligand for Lactose-Binding Protein: Implications for Early Detection of Pancreatic Carcinomas with PET.
MedLine Citation:
PMID:  20593279     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
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'-[(18)F]fluoro-β-D: -glucopyranoside (Et-[(18)F]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-[(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-[(18)F]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-[(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.
CONCLUSION: These results suggest that Et-[(18)F]FDL is a promising agent which should be evaluated for detection of early pancreatic carcinomas by PET/CT imaging.
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
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging     Volume:  13     ISSN:  1860-2002     ISO Abbreviation:  Mol Imaging Biol     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-05-05     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101125610     Medline TA:  Mol Imaging Biol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  536-46     Citation Subset:  IM    
Affiliation:
Department of Experimental Diagnostic Imaging, Center for Advanced Biomedical Imaging Research (CABIR), The University of Texas MD Anderson Cancer Center, 1881 East Road, 3SCR2.3924, Houston, TX, 77030, USA.
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