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.
abstract: BACKGROUND
  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.
  
  
  CONCLUSIONS
  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.
  
  
  CONCLUSIONS
  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.
authors.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.
authors.forename: Yunming
authors.initials: Y
authors.lastname: Ying
authors.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.
authors.forename: Pradip
authors.initials: P
authors.lastname: Ghosh
authors.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.
authors.forename: Liwei
authors.initials: L
authors.lastname: Guo
authors.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.
authors.forename: Ashutosh
authors.initials: A
authors.lastname: Pal
authors.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.
authors.forename: Uday
authors.initials: U
authors.lastname: Mukhapadhyay
authors.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.
authors.forename: Zhenghong
authors.initials: Z
authors.lastname: Peng
authors.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.
authors.forename: Hsin Hsien
authors.initials: HH
authors.lastname: Yeh
authors.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.
authors.forename: Susanna
authors.initials: S
authors.lastname: Bertolini
authors.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.
authors.forename: Leo Garcia
authors.initials: LG
authors.lastname: Flores
authors.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.
authors.forename: Daniel
authors.initials: D
authors.lastname: Young
authors.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.
authors.forename: Andrei
authors.initials: A
authors.lastname: Volgin
authors.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.
authors.forename: Suren
authors.initials: S
authors.lastname: Soghomonyan
authors.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.
authors.forename: William
authors.initials: W
authors.lastname: Bornmann
authors.affiliation: Department of Cancer Biology, The University of Texas MD Anderson Cancer Center, Houston, TX, USA.
authors.forename: Craig
authors.initials: C
authors.lastname: Logsdon
authors.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.
authors.forename: Mian M
authors.initials: MM
authors.lastname: Alauddin
authors.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. jgelovani@mdanderson.org.
authors.forename: Juri G
authors.initials: JG
authors.lastname: Gelovani
mesh_terms: D000818:Animals; D000951:Antigens, Neoplasm / Q000378:metabolism; D001345:Autoradiography / Q000379:methods*; D014408:Biomarkers, Tumor / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D004187:Disaccharides / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D055088:Early Detection of Cancer; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification; D054879:Halogenation; D007150:Immunohistochemistry; D007785:Lactose / Q000378:metabolism*; D037181:Lectins, C-Type / Q000378:metabolism; D008024:Ligands; D051379:Mice; D009363:Neoplasm Proteins / Q000378:metabolism*; D010190:Pancreatic Neoplasms / Q000000981:diagnostic imaging*; D000073718:Pancreatitis-Associated Proteins; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D000951:Antigens, Neoplasm; D014408:Biomarkers, Tumor; D004187:Disaccharides; D005960:Glucosides; D037181:Lectins, C-Type; D008024:Ligands; D009363:Neoplasm Proteins; D000073718:Pancreatitis-Associated Proteins; C000612141:REG3A protein, human; D019275:Radiopharmaceuticals; C560565:ethyl galactopyranosyl-(1-4)-2'-deoxy-2'-fluoroglucopyranoside; D007785:Lactose