Highly potent inhibitors of the Grb2-SH2 domain

被引：51

作者：

Schoepfer, J ^{[1
]}

Fretz, H ^{[1
]}

Gay, B ^{[1
]}

Furet, P ^{[1
]}

García-Echeverría, C ^{[1
]}

End, N ^{[1
]}

Caravatti, G ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(98)00701-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Highly potent inhibitors of the Grb2-SH2 domain have been synthesized. They share the common sequence: Ac-Pmp-Ac(6)c-Asn-NH-(3-indolyl-propyl). Different substituents at the 3-indolyl-propylamine C-terminal group were explored to further improve the activity. This is the first example of inhibitors of SH2 domains with sub-nanomolar affinity reported to date. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：221 / 226

页数：6

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