FMRFamide-related neuropeptides are agonists of the orphan G-protein-coupled receptor GPR54
FMRFamide-related neuropeptides are agonists of the orphan G-protein-coupled receptor GPR54
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DOI：
10.1006/bbrc.2001.5098
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发表时间：
2001-06-29
影响因子：
3.1
通讯作者：
Liu, QY
中科院分区：
文献类型：
--
作者：
Clements, MK;McDonald, TP;Liu, QY
我们已经分离并测定了大鼠孤儿G蛋白偶联受体GPR54的人和小鼠同源基因的编码序列。小鼠和大鼠GPR54的同源性接近95%，在氨基酸水平上与人GPR54的同源性约为85%。对GPR54激动剂的筛选发现，RFamide和RWamide家族中的几个无脊椎动物神经肽能够通过G(αq)途径在最大范围内激活GPR54。取代分析表明，GPr54-激活肽的C端最佳序列为Gly-Leu-Arg-Trp-NH2。Northern分析发现，人类GPr54在几个外周组织和中枢神经系统的许多区域都有表达。(C)2001年学术出版社。
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.