PHENYLALKYL KETONES AS POTENT REVERSIBLE INHIBITORS OF INTERLEUKIN-1-BETA CONVERTING-ENZYME

被引：27

作者：

MJALLI, AMM ^{[1
]}

CHAPMAN, KT ^{[1
]}

MACCOSS, M ^{[1
]}

THORNBERRY, NA ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,DEPT BIOCHEM,RAHWAY,NJ 07065

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 12期

关键词：

D O I：

10.1016/S0960-894X(01)80743-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Phenylalkyl ketones are potent reversible inhibitors of interleukin-1beta converting enzyme (ICE). The extended alkyl chain ketones AcTyrValAlaAspCO(CH2)nPh display increased potency over the simple aryl ketone. In particular, the tetrapeptide AcTyrValAlaAspCOPh has a K(i) of 10muM while AcTyrValAlaAspCO(CH2)5Ph has a K(i) of 18.5nM.

引用

页码：2689 / 2692

页数：4

共 11 条

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