Journal
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
Volume 464, Issue 3, Pages 743-747Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bbrc.2015.07.020
Keywords
GPR64; GPCR; G protein; Molecular pharmacology; Signal transduction; Peptide agonist
Categories
Funding
- Deutsche Forschungsgemeinschaft [FOR2149]
- Bundesministerium fur Forschung und Bildung (IFB AdipositasDiseases Leipzig) [K7-67]
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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.
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