Structure-activity relationship of linear peptide Bu-His-DPhe-Arg-Trp-Gly-NH2 at the human melanocortin-1 and-4 receptors:: Arginine substitution

被引：33

作者：

Cheung, AWH ^{[1
]}

Danho, W ^{[1
]}

Swistok, J ^{[1
]}

Qi, L ^{[1
]}

Kurylko, G ^{[1
]}

Franco, L ^{[1
]}

Yagaloff, K ^{[1
]}

Chen, L ^{[1
]}

机构：

[1] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 17期

关键词：

D O I：

10.1016/S0960-894X(02)00459-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of pentapeptides, based on Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH2 and modified at the Arg(8) position, was prepared and pharmacologically characterized. Peptides containing either cyanoguanidine or acylguanidine, two substantially less basic arginine surrogates, were found to retain the agonist activity of the parent peptide at both hMC1R and hMC4R. This study unequivocally shows that the positive charge of Arg(8) is not essential for efficient interactions of our pentapeptide with both hMC1R and hMC4R. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2407 / 2410

页数：4

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