New syntheses of tetrazolylmethylphenylaianine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors

被引：17

作者：

Dourlat, Jennifer

Valentin, Bruno

Liu, Wang-Qing

Garbay, Christiane ^{[1
]}

机构：

[1] Univ Paris 05, UFR Biomed, Lab Pharmacochim Mol & Cellulaire, F-75006 Paris, France

[2] INSERM, U648, F-75006 Paris, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期

关键词：

STAT3; pTyr mimetics; inhibitors; SH2; domain; cancer;

D O I：

10.1016/j.bmcl.2007.04.107

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Investigation within the pTyr-binding pocket of the STAT3 SH2 domain led us to develop a novel synthesis of two pTyr mimetics, L-tetrazolylmethylphenylalanine (L-Tmp) and L-O-malonyltyrosine (L-OMT), that were next incorporated in a high affinity ligand of STAT3 SH2 domain. Biological evaluation of peptidomimetics on STAT3 dimerization identified L-OMT as the first non-phosphorus pTyr mimetic so far reported against STAT3 SH2 domain, harboring an activity similar to that of the Pmp-containing reference peptidomimetic. (C) 2007 Elsevier Ltd. All rights reserved.

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页码：3943 / 3946

页数：4

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