THE SYNTHESIS AND EVALUATION OF PEPTIDYL ASPARTYL ALDEHYDES AS INHIBITORS OF ICE

Authors
MULLICAN MD LAUFFER DJ GILLESPIE RJ MATHARU SS KAY D PORRITT GM EVANS PL GOLEC JMC MURCKO MA LUONG YP RAYBUCK SA LIVINGSTON DJ
Citation
Md. Mullican et al., THE SYNTHESIS AND EVALUATION OF PEPTIDYL ASPARTYL ALDEHYDES AS INHIBITORS OF ICE, Bioorganic & medicinal chemistry letters, 4(19), 1994, pp. 2359-2364
Citations number
14
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
4
Issue
19
Year of publication
1994
Pages
2359 - 2364
Database
ISI
SICI code
0960-894X(1994)4:19<2359:TSAEOP>2.0.ZU;2-9
Abstract
The tetrapeptide aldehyde Ac-Tyr-Val-Ala-AspH (1, L709,049) has been r eported to be a potent reversible inhibitor of Interleukin-1 beta Conv erting Enzyme (ICE). We have prepared a series of analogs of 1, in ord er to explore the active site of ICE. The effects of truncation, methy lation of the amide nitrogens and modification of the aldehyde group o f 1 are presented.