Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor

被引：61
|
作者：
Darker, JG
Porter, RA
Eggleston, DS
Smart, D
Brough, SJ
Sabido-David, C
Jerman, JC
机构：
[1] SmithKline Beecham Pharmaceut, Discovery Chem, Harlow CM19 5AW, Essex, England
[2] SmithKline Beecham Pharmaceut, Neurosci Res, Harlow CM19 5AW, Essex, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 05期
关键词：
D O I：
10.1016/S0960-894X(01)00043-9
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Truncated peptide analogues of orexin-A were prepared and their biological activity assesed at the orexin-1 receptor. Progressive N-terminal deletions identified the minimum C-terminal sequence required for maintaining a significant agonist effect, whilst an alanine scan and other pertinent substitutions identified key side-chain and stereochemical requirements for receptor activation. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：737 / 740
页数：4
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