Introduction of GPR62
Probable G-protein coupled receptor 62, also known as G-protein coupled receptor GPCR8 or hGPCR8, is a protein that in humans is encoded by the GPR62 gene. As a member of the G protein-coupled receptors family, GPR62 contains 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins. During the past years, the functions and applications of GPR62 have been widely studied.
|Basic Information of GPR62|
|Protein Name||Putative G-protein coupled receptor GPR62|
G-protein coupled receptor GPCR8, hGPCR8, G-protein coupled receptor
|Organism||Homo sapiens (Human)|
Function of GPR62 Membrane Protein
G-protein-coupled receptors (GPCRs) participate in diverse physiological functions and are promising targets for drug discovery. Studies have shown that over 140 orphan GPCRs whose functions remain to be elucidated. As a member of the orphan GPCRs, GPR62 is reported to be expressed in the rat and human brain. It has also found that GPR62 is expressed in male germ cells in mice and its expression increases along with sperm differentiation. Most importantly, studies have shown that expression of increasing amounts of GPR62 could increase cAMP levels suggesting that GPR62 is constitutively active on the Gs/cAMP pathway. What’s more, inositol phosphate (IP1) production will increase in a dose-dependent manner up to 40% in cells expressing HA-GPR62. It indicates that GPR62 is constitutively active on the Gq/IP1 pathway in HEK293T cells.
Fig.1 Cross talk between melatonin receptors and orphan GPCRs. (Oishi, 2018)
Application of GPR62 Membrane Protein in Literature
This article suggests that GPR62 could constitutively activate the cAMP pathway in male germ cells but is dispensable for male fertility, which is probably due to its functional redundancy with GPR61.
This article suggests that GPR62 could not bind melatonin, but show a reciprocal regulatory interaction with MT2 receptors.
This article aims to evaluate the extent of constitutive activity among orphan class-A G protein-coupled receptors within the cAMP signaling pathway. It suggests that identification of inverse agonists may be a fruitful approach for categorizing these orphan receptors and targeting them for pharmacological intervention.
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