True interaction mode of porcine pancreatic elastase with FR136706, a potent peptidyl inhibitor

被引：9
作者：
Kinoshita, T [1 ]
Nakanishi, I
Sato, A
Tada, T
机构：
[1] Fujisawa Pharmaceut Co Ltd, Exploratory Res Labs, Tsukuba, Ibaraki 3002698, Japan
[2] Fujisawa Pharmaceut Co Ltd, Analyt Res Labs, Tsukuba, Ibaraki 3002698, Japan
[3] Univ Osaka Prefecture, Res Inst Adv Sci & Technol, Sakai, Osaka 2938570, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 01期
关键词：
D O I：
10.1016/S0960-894X(02)00852-1
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The crystal structure of porcine pancreatic elastase (PPE) complexed with a potent peptidyl inhibitor FR136706, was solved at 2.2Angstrom resolution. FR136706 fits snugly into the extended active site pocket. The benzene moiety of FR136706 induced dramatic movement of the side chain moiety of Arg217 and both moieties formed a pi-pi interaction, which has never been found previously in structures of PPE complexed with inhibitors. This novel interaction mode may lead to design of new types of inhibitors. (C) 2002 Elsevier Science Ltd. All rights reserved.
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页码：21 / 24
页数：4
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