GPR31
| GPR31 | |||||||||||||||||
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| Aliases | GPR31, 12-HETER, HETER, HETER1, G protein-coupled receptor 31 | ||||||||||||||||
| External IDs | MGI: 1354372 HomoloGene: 48337 GeneCards: GPR31 | ||||||||||||||||
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| Species | Human | Mouse | |||||||||||||||
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| Location (UCSC) | Chr 6: 167.16 – 167.16 Mb | Chr 17: 13.05 – 13.05 Mb | |||||||||||||||
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G-protein coupled receptor 31 also known as 12-(S)-HETE receptor is a protein that in humans is encoded by the GPR31 gene. The human gene is located on chromosome 6q27 and encodes a G-protein coupled receptor protein composed of 319 amino acids.
The GPR31 receptor is most closely related in amino acid sequence to the oxoeicosanoid receptor 1, a G-protein coupled receptor encoded by the GPR170 gene. Oxoeicosanoid receptor 1 is the receptor for a family of arachidonic acid metabolites made by 5-lipoxygenase viz., 5-Hydroxyicosatetraenoic acid (5-HETE), 5-oxoicosanoic acid (5-oxo-ETE) and other members of this family of broadly bioactive cell stimuli. The GPR31 receptor is a receptor for very different arachidonic acid metabolite, 12-hydroxyeicosatetraenoic acid (12-HETE), whose synthesis is catalyzed by 12-lipoxygenase; this conclusion is based on studies that cloned the receptor from the PC-3 prostate cancer cell line and found that the cloned receptor, when expressed in other cell types, bound with high affinity (Kd=5 nM) and mediated the actions of low concentrations of the S but not R stereoisomer of 12-HETE. In a [35S]GTPγS binding assay, which indirectly estimates a receptor's binding affinity with a ligand by measuring this ligand's ability to stimulate the receptor to bind [35S]GTPγS, 12(S)-HETE stimulated the cloned GPR31 receptor to bind [35S]GTPγS with an EC50 (effective concentration causing a 50% of maximal rise in [35S]GTPγS binding) was <0.3 nM; it was 42 nm for 15(S)-HETE, 390 nM for 5(S)-HETE, and undetectable for 12(R)-HETE. Importantly, however, we do not known if GPR31 interacts with structural analogs of 12(S)-HETE such as 12-oxo-ETE (a metabolite of 12(S)-HETE), various 5,12-diHETEs including LTB4, and an array of bioactive 12(S)-HETE and 12(R)-HETE metabolites, the Hepoxilins. Further studies will be needed to determine if the GPR31 receptor is dedicated to binding and mediating the aciont of 12(S)-HETE more or less exclusively or, like the oxoeicosanoid receptor 1, binds and mediates the actions of a family of analogs.
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Wikipedia