Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo αvβ3 integrin related tumor imaging

被引：60

作者：

Ogawa, M

Hatano, K ^{[1
]}

Oishi, S

Kawasumi, Y

Fujii, N

Kawaguchi, M

Doi, R

Imamura, M

Yamamoto, M

Ajito, K

Mukai, T

Saji, H

Ito, K

机构：

[1] Natl Inst Longev Sci, Dept Biofunct Res, Morioka, Obu 4748522, Japan

[2] Kyoto Univ, Dept Bioorgan Med Chem, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

[3] Kyoto Univ, Dept Surg & Surg Basic Sci, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

[4] Meiji Seika Kaisha Ltd, Pharmaceut Res Ctr, Kohoku Ku, Yokohama, Kanagawa 2228567, Japan

[5] Kyoto Univ, Dept Nucl Med & Diagnost Imaging, Grad Sch Med, Sakyo Ku, Kyoto 6068501, Japan

[6] Kyoto Univ, Dept Pathofunct Bioanal, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2003年 / 30卷 / 01期

基金：

日本学术振兴会;

关键词：

fluorine-18; radiofluorination; RGD peptide; alpha(v)beta(3) integrin; tumor imaging;

D O I：

10.1016/S0969-8051(02)00387-6

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：

The association of the alpha(v)beta(3) integrin with tumor metastasis and tumor related angiogenesis has been suggested. Therefore, by imaging the alpha(v)6(3) receptor with PET. information concerning the tumor status could be obtained. Cyclic peptides including the RGD sequence. Were radiolabeled by direct electrophilic fluorination with [F-18]AcOF. In tumor-bearing mice, the labeled peptides accumulated at the tumor with a high tumor to blood ratio. These findings suggest that an assessment of tumor characteristics may be obtained by using these F-18-labeled peptides. (C) 2002 Elsevier Science Inc. All rights reserved.

引用

页码：1 / 9

页数：9

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