FMRFamide-related neuropeptides are agonists of the orphan G-protein-coupled receptor GPR54

被引:95
作者
Clements, MK
McDonald, TP
Wang, RP
Xie, GC
O'Dowd, BF
George, SR
Austin, CP
Liu, QY
机构
[1] Merck Res Labs, Dept Pharmacol, W Point, PA 19486 USA
[2] Merck Res Labs, Dept Bioinformat, W Point, PA 19486 USA
[3] Univ Toronto, Dept Pharmacol, Toronto, ON M5S 1A8, Canada
关键词
D O I
10.1006/bbrc.2001.5098
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
We have isolated and determined the coding sequences of human and mouse orthologs of the rat orphan G-protein-coupled receptor GPR54. Mouse and rat GPR54 are nearly 95% identical to each other, and both are approximately 85% identical to human GPR54 at the amino acid level. Screening of agonists for GPR54 identified several invertebrate neuropeptides of the RFamide and RWamide family that were able to activate GPR54 at muM range through the G(alphaq) pathway. Substitution analysis showed that the C-terminal optimal sequence of GPR54-activating peptides is Gly-Leu-Arg-Trp-NH2. Northern analysis of human GPR54 detected expression in several peripheral tissues and many regions of the central nervous system. (C) 2001 Academic Press.
引用
收藏
页码:1189 / 1193
页数:5
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