Identification of the tethered peptide agonist of the adhesion G protein-coupled receptor GPR64/ADGRG2
Identification of the tethered peptide agonist of the adhesion G protein-coupled receptor GPR64/ADGRG2
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DOI：
10.1016/j.bbrc.2015.07.020
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发表时间：
2015-08-28
影响因子：
3.1
通讯作者：
Liebscher, Ines
中科院分区：
文献类型：
--
作者：
Demberg, Lilian M.;Rothemund, Sven;Liebscher, Ines
附睾特异性粘附G蛋白偶联受体（aGPCR）GPR 64/ADGRG 2已被证明是男性生殖系统的关键参与者。由于GPR 64的破坏导致不育，因此GPR 64作为男性生育控制或改善的潜在靶点引起了人们的关注。与大多数aGPCR一样，GPR 64在其内源性激动剂和信号转导方面是孤儿受体。在这项研究中，我们研究了GPR 64的G蛋白偶联能力，并表明它是通过一个拴系激动剂序列激活的，我们以前已经确定为Stachel序列。来自Stachel区域的合成肽可以激活受体，首次打开了外部操纵受体活性的可能性。(C)2015 Elsevier Inc. All rights reserved.
The epididymis-specific adhesion G protein-coupled receptor (aGPCR) GPR64/ADGRG2 has been shown to be a key-player in the male reproductive system. As its disruption leads to infertility, GPR64 has drawn attention as potential target for male fertility control or improvement. Like the majority of aGPCRs GPR64 is an orphan receptor regarding its endogenous agonist and signal transduction. In this study we examined the G protein-coupling abilities of GPR64 and showed that it is activated through a tethered agonist sequence, which we have previously identified as the Stachel sequence. Synthetic peptides derived from the Stachel region can activate the receptor, opening for the first time the possibility to externally manipulate the receptor activity. (C) 2015 Elsevier Inc. All rights reserved.