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

被引：12

作者：

Ying, Yunming ^{[1
]}

Ghosh, Pradip ^{[1
]}

Guo, Liwei ^{[1
]}

Pal, Ashutosh ^{[1
]}

Mukhapadhyay, Uday ^{[1
]}

Peng, Zhenghong ^{[1
]}

Yeh, Hsin Hsien ^{[1
]}

Bertolini, Susanna ^{[1
]}

Flores, Leo Garcia ^{[1
]}

Young, Daniel ^{[1
]}

Volgin, Andrei ^{[1
]}

Soghomonyan, Suren ^{[1
]}

Bornmann, William ^{[1
]}

Logsdon, Craig ^{[2
]}

Alauddin, Mian M. ^{[1
]}

Gelovani, Juri G. ^{[1
]}

机构：

[1] Univ Texas MD Anderson Canc Ctr, Ctr Adv Biomed Imaging Res CABIR, Dept Expt Diagnost Imaging, Houston, TX 77030 USA

[2] Univ Texas MD Anderson Canc Ctr, Dept Canc Biol, Houston, TX 77030 USA

来源：

MOLECULAR IMAGING AND BIOLOGY | 2011年 / 13卷 / 03期

关键词：

Fluorine-18; Lactose; HIP/PAP protein; Pancreatic carcinoma; PET; PRIMARY LIVER-CANCER; DUCTAL ADENOCARCINOMA; GENE; INTESTINE; PLASMA; MICE;

D O I：

10.1007/s11307-010-0334-9

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

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-beta-d-galactopyranosyl-(1,4')-2'-deoxy-2'-[F-18]fluoro-beta-d-glucopyranoside (Et-[F-18]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-[F-18]FDL produced no isomers; the average decay-corrected radiochemical yield was 68%, radiochemical purity > 99%, and specific activity > 74 GBq/A mu mol. The radioligand properties of Et-[F-18]FDL were evaluated using an ex vivo autoradiography and immunohistochemistry in pancreatic tissue sections obtained from mice-bearing orthotopic pancreatic tumor xenografts. Et-[F-18]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-[F-18]FDL is a promising agent which should be evaluated for detection of early pancreatic carcinomas by PET/CT imaging.

引用

页码：536 / 546

页数：11

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