18F-labelling of a cyclic pentapeptide inhibitor of the chemokine receptor CXCR4

被引：13

作者：

Aberg, Ola ^{[1
]}

Pisaneschi, Federica ^{[1
]}

Smith, Graham ^{[1
]}

Quang-De Nguyen ^{[1
]}

Stevens, Elizabeth ^{[1
]}

Aboagye, Eric O. ^{[1
]}

机构：

[1] Univ London Imperial Coll Sci Technol & Med, Hammersmith Hosp, Fac Med, Comprehens Canc Imaging Ctr,Dept Surg & Canc, London W12 0NN, England

来源：

JOURNAL OF FLUORINE CHEMISTRY | 2012年 / 135卷

基金：

英国医学研究理事会; 英国工程与自然科学研究理事会;

关键词：

CXCR4; Cyclic pentapeptide; PET imaging; F-18]fluorobenzaldehyde; Radiolabelling; POSITRON-EMISSION-TOMOGRAPHY; BREAST-CANCER METASTASIS; SMALL-MOLECULE; ANTAGONIST; F-18; PEPTIDES; PET; IDENTIFICATION; EXPRESSION; FLUORIDES;

D O I：

10.1016/j.jfluchem.2011.11.003

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

The chemokine receptor CXCR4 is overexpressed in a variety of cancers including breast, prostate and lung cancer. Expression is also associated with invasion and metastasis. The possibility to image and quantify CXCR4 expression in vivo would be a valuable tool in the clinic to aid treatment regimens and to potentially understand the underlying biology of metastasis. Herein we describe the synthesis and the radiolabelling of an F-18-labelled cyclic pentapeptide, [F-18]CCIC-0007 designed to bind to the extracellular domains of CXCR4. Radiolabelling was performed via conjugation of [F-18]fluorobenzaldehyde with an aminooxy functionalised cyclopentapeptide. Typically, starting with 1.10 GBq (30 mCi) of aqueous [F-18]fluoride, 105 MBq (2.85 mCi) of the formulated tracer was obtained within 2.5 h (23 +/- 8% dc rcy, 8% EOS yield). Tissue pharmacokinetic studies in mice demonstrated rapid blood clearance, together with biliary and renal elimination. (C) 2011 Elsevier B.V. All rights reserved.

引用

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页码：200 / 206

页数：7

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