High impact information on GPR6

• In summary, our data suggest that gpr3, gpr6 and gpr12 are a family of constitutively active receptors with dual coupling to G(alpha)(s) and G(alpha)(i) type of G proteins [1].
• When expressed transiently in HEK293 cells, gpr3, gpr6 and gpr12 confer constitutive activation of adenylate cyclase (AC) similar in amplitude to that seen with fully activated G(alpha)(s)-coupled receptors [1].
• In CHO cells transfected with GPR6, the sphingosine-kinase pathway mediated Ca(2+) mobilization from internal stores [2].
• The GPR6 gene was found to be located on chromosome 10B1 and a single exon coded for the entire open-reading frame [2].
• Fluid shear stress differentially regulates gpr3, gpr6, and gpr12 expression in human umbilical vein endothelial cells [3].

Biological context of GPR6

• Gene GPR6 encoded a receptor that shared closest identity (71% in the transmembrane regions) with the human orphan receptor GPR3 and was localized to chromosome 6 (q21-q22.1) [4].

Anatomical context of GPR6

• Northern blot analysis revealed that GPR6 transcripts were abundant in the human putamen and to a lesser extent in the frontal cortex, hippocampus, and hypothalamus [4].
• We next sought to determine the role of fluid shear stress in the regulation of expression of gpr3, gpr6 and gpr12 by using human umbilical vein endothelial cells (HUVECs) [3].

Associations of GPR6 with chemical compounds

• Sphingosine-1-phosphate (S1P) activated GPR6, transiently expressed in frog oocytes or in Chinese hamster ovary (CHO) cells, with high specificity and nanomolar affinity [2].

Analytical, diagnostic and therapeutic context of GPR6

• Fluorescence in situ hybridization of GPR12, GPR6, and GPR3 localized these three genes to human chromosomal regions 13q12, 6q21, and 1p34.3-p36.1, respectively [5].
• In contrast, gpr3 and gpr12 protein were increased after 12 hrs of shear stress by 95% and 40%, respectively. gpr6 mRNA and protein were absent in HUVECs as determined by Taqman and western blot techniques [3].

References