Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2
Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2
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DOI：
10.1016/s0960-894x(99)00299-1
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发表时间：
1999-07-19
影响因子：
2.7
通讯作者：
Furet, P
中科院分区：
文献类型：
--
作者：
Caravatti, G;Rahuel, J;Furet, P
基于结构的设计和合成了一种完全非肽的Grb2 SH2结构域的微摩尔拮抗剂。该化合物模拟了天然配体的两个主要药效团，即磷酸酪氨酸残基的苯磷酸盐和X+2天冬酰胺的β -羧酰胺，它们由刚性芳香间隔物连接。1999爱思唯尔科学有限公司版权所有。
The structure-based design and synthesis of a completely non-peptidic, micromolar antagonist of the SH2 domain of Grb2 is presented. The compound mimics the two main pharmacophores of the natural ligand, the phenylphosphate of the phosphotyrosine residue and the beta-carboxamide of the X+2 asparagine, which are linked by a rigid aromatic spacer. (C) 1999 Elsevier Science Ltd. All rights reserved.