Spatial requirements of the antagonist binding site of the NK2 receptor

被引：14

作者：

Ali, MA

Bhogal, N

Fishwick, CWG ^{[1
]}

Findlay, JBC

机构：

[1] Univ Leeds, Sch Chem, Leeds LS2 9JT, W Yorkshire, England

[2] Univ Leeds, Sch Biochem & Mol Biol, Leeds LS2 9JT, W Yorkshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 06期

基金：

英国工程与自然科学研究理事会;

关键词：

D O I：

10.1016/S0960-894X(01)00074-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Computer-aided modelling has been used to identify a putative antagonist binding site in the tachykinin NK2 receptor. In order to validate the implied spatial requirements for this region, a series of compounds, based on the potent antagonist GR 149861 have been synthesised and their binding affinities established. Our findings suggest the presence of a large hydrophobic cavity in the putative binding crevice of GR 149861. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：819 / 822

页数：4

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