New syntheses of tetrazolylmethylphenylaianine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors
New syntheses of tetrazolylmethylphenylaianine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors
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DOI：
10.1016/j.bmcl.2007.04.107
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发表时间：
2007-07-15
影响因子：
2.7
通讯作者：
Garbay, Christiane
中科院分区：
文献类型：
--
作者：
Dourlat, Jennifer;Valentin, Bruno;Garbay, Christiane
在STAT 3 SH 2结构域的pTyr结合口袋内的研究使我们开发了两种pTyr模拟物，L-四唑基甲基苯丙氨酸（L-Tmp）和L-O-丙二酰酪氨酸（L-OMT）的新合成，它们接下来被并入STAT 3 SH 2结构域的高亲和力配体中。肽模拟物对STAT 3二聚化的生物学评价鉴定了L-OMT作为迄今为止报道的针对STAT 3 SH 2结构域的第一个非磷pTyr模拟物，其具有与含有Pmp的参考肽模拟物类似的活性。(C)2007爱思唯尔有限公司保留所有权利。
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.