Introduction of GPRC6A
GPRC6A is a member of the family C G protein-coupled receptors, which are characterized by the presence of a seven-transmembrane domain and an unusually long amino-terminal domain (ATD). This receptor was initially deorphanized by infusion of its large N-terminal domain to the heptahelical and C-terminal region of the related goldfish 5.24 receptor. Cell signaling studies suggest that the receptor couples primarily via the Gαq/11 pathway to increase inositol phosphate production and mobilize intracellular calcium. Besides, it may also increase cyclic AMP and/or phosphorylation of extracellular signal-regulated kinase-1/2.
|Basic Information of GPRC6A|
|Protein Name||G-protein coupled family C group 6 member A|
|Organism||Homo sapiens (Human)|
Functions of GPRC6A Membrane Protein
This receptor has a broad expression in brain and peripheral tissues with highest levels in kidney, skeletal muscle, testis, and leucocytes. It functions via binding to different ligands, including L-α-amino acids, divalent cations, osteocalcin, and steroids. However, the broad ligand recognition and tissue expression have obscured the elucidation of the specific physiological role of this receptor and the mechanisms regulating its activity and cell surface availability. Studies in GPRC6A knockout mice have revealed that loss-of-CPRC6A results in metabolic syndrome. Moreover, bone, cardiovascular, immune, and skin functions of GPRC6A have also been identified in mice. However, the function of this receptor in humans remains unclear.
Applications of GPRC6A in Literature
The study demonstrated that GPRC6A was not necessary for the effects of low- and high-protein diets on body weight and food intake in mice.
This study investigated the role of GPRC6A in Alum adjuvanticity. Results showed that Alum adjuvanticity is increased in GPRC61-deficient mice, suggesting that GPRC6A limited the humoral response to Alum.
This article studied the agonist of GPRC6A (de-carboxylatedosteocalcin) in cells and found that the reported mouse GPRC6A-dependent effects of OCN may result from indirect, rather than direct activation of the receptor.
This article presented the structure-activity relationship study of the 2-arylindole antagonist 3 of GPRC6A, including the design, synthesis, and pharmacological information.
This article studied the possible association between rs2274911 polymorphism and male fertility and/or cryptorchidism. The results suggested that GPRC6A inactivation or sub-function contributed to reduced exposure to androgens, resulting in cryptorchidism during fetal life and/or low sperm production in adulthood.
GPRC6A Preparation Options
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