Structure-based design of a non-peptidic antagonist of the SH2 domain of Grb2

被引：19

作者：

Caravatti, G ^{[1
]}

Rahuel, J ^{[1
]}

Gay, B ^{[1
]}

Furet, P ^{[1
]}

机构：

[1] Novartis Pharmaceut Inc, Therapeut Area Oncol, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(99)00299-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

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页数：6

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