Synthesis, in vitro screening and in vivo evaluation of cyclic RGD analogs cyclized through. oxorhenium and oxotechnetium coordination

被引：6

作者：

Aufort, Marie ^{[1
]}

Gonera, Marta ^{[1
]}

Lelait, Marie-Anne ^{[1
]}

Czarny, Bertrand ^{[1
]}

Le Clainche, Loic ^{[1
]}

Thai, Robert ^{[1
]}

Landra, Amandine ^{[1
]}

de Brimont, Mathias Ruinart ^{[1
]}

Dugave, Christophe ^{[1
]}

机构：

[1] CEA Saclay, iBiTec S SIMOPRO, F-91191 Gif Sur Yvette, France

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 05期

关键词：

Integrin; RGD; Angiogenesis; Rhenium; Technetium; Cyclopeptide; CYCLOPHILIN HCYP-18 LIGANDS; BACKBONE METAL-CYCLIZATION; BIOLOGICAL EVALUATION; INTEGRIN LIGANDS; INITIAL EVALUATION; RHENIUM; PEPTIDES; EXPRESSION; MICROPET; COMPLEX;

D O I：

10.1016/j.ejmech.2011.02.032

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A library of RGD tripeptide analogs cyclized through oxorhenium coordination by an NS2/S chelation motif was synthesized. Screening towards integrins alpha V beta 3, alpha llb beta 3 and alpha V beta 5 led to the identification of 6 oxorhenium complexes that bind to integrin alpha V beta 3 in the submicromolar range. In vivo evaluation of five of the corresponding oxotechnetium complexes using nude mice bearing a U87MG human tumor xenograft showed a significant and specific accumulation of radioactivity inside the tumor. The best results in vivo were obtained with complexes Tc-16 and Tc-50 that displayed a higher tumor accumulation and a lower distribution in other tissues relative to a reference cyclopentapeptide tracer. (C) 2011 Elsevier Masson SAS. All rights reserved.

引用

页码：1779 / 1788

页数：10

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