Peptide Based Interleukin-1. BETA. Converting Enzyme (ICE) Inhibitors: Synthesis, Structure Activity Relationships and Crystallographic Study of the ICE-inhibitor …

…, Y YONETOKU, H KURIHARA, H SAKASHITA…

Index: Okamoto, Yoshinori; Anan, Hideki; Nakai, Eiichi; Morihira, Koichiro; Yonetoku, Yasuhiro; Kurihara, Hiroyuki; Sakashita, Hitoshi; Terai, Yoshiya; Takeuchi, Makoto; Shibanuma, Tadao; Isomura, Yasuo Chemical and Pharmaceutical Bulletin, 1999 , vol. 47, # 1 p. 11 - 21

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Citation Number: 51

Abstract

Based on the X-ray structure of the complex of Ac-Tyr-Val-Ala-Asp-H (L-709049) and interleukin-1β converting enzyme (ICE), we synthesized compounds which were derived from 2-NapCO-Val-Pro-Asp-CH 2 OPh (1) to obtain a potent inhibitor in the cell assay. Among these compounds,(3S)-N-methanesulfonyl-3-[[1-[N-(2-naphthoyl)-L-valyl]-L-prolyl] amino]-4-oxobutanamide (27c) showed high potency not only in the enzyme assay but ...