Structure-based design of peptidomimetic ligands of the Grb2-SH2 domain

被引：24

作者：

Schoepfer, J ^{[1
]}

Gay, B ^{[1
]}

Caravatti, G ^{[1
]}

Garcia-Echeverria, C ^{[1
]}

Fretz, H ^{[1
]}

Rahuel, J ^{[1
]}

Furet, P ^{[1
]}

机构：

[1] Novartis Pharma Inc, Oncol Res Dept, CH-4002 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(98)00513-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have designed and synthesized a (3-aminomethyl-phenyl)-urea scaffold to mimic the X+1-Asn part of the minimal phosphopeptide sequence, Ac-pTyr-X+1-Asn-NH2, recognized by the Grb2-SH2 domain. The resulting compounds show the same degree of affinity as their peptide counterparts for the Grb2-SH2 domain. This is the first example reported to date of ligands of the Grb2-SH2 domain with substantially reduced peptidic character. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2865 / 2870

页数：6

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