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

被引：62

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

页码：737 / 740

页数：4

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