Conformationally constrained inhibitors of caspase-1 (interleukin-1β converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain)

被引：48

作者：

Karanewsky, DS ^{[1
]}

Bai, X ^{[1
]}

Linton, SD ^{[1
]}

Krebs, JF ^{[1
]}

Wu, J ^{[1
]}

Pham, B ^{[1
]}

Tomaselli, KJ ^{[1
]}

机构：

[1] Idun Pharmaceut, La Jolla, CA 92037 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00498-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A systematic study of interleukin-lp converting enzyme (ICE, caspase-1) and caspase-3 (CPP32, apopain) inhibitors incorporating a PGammaP3 conformationally constrained dipeptide mimetic is reported. Depending on the nature of the P-4 substituent, highly selective inhibitors of both Csp-l or Csp-3 were obtained. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：2757 / 2762

页数：6

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