GPR109A

GPR109A

GPR109A is a nicotinate-specific G protein-coupled receptor, but it only has a weak affinity for butyrate. The lumen-facing apical membrane of intestinal and colonic epithelial cells express GPR109A, and the receptor recognizes butyrate as a ligand. GPR109A is not expressed in human colon cancer, intestinal/colon cancer mouse models, or colon cancer cell lines. DNA methylation is either directly or indirectly involved in the tumor-associated silencing of GPR109A. Reexpressing GPR109A causes apoptosis in colon cancer cells, but only when its ligands butyrate and nicotinate are present.Although butyrate inhibits histone deacetylases, activating GPR109A with its ligands causes apoptosis in colon cancer cells that does not involve inhibition of histone deacetylation. The main alterations in this apoptotic process are the up-regulation of the death receptor pathway and the down-regulation of Bcl-2, Bcl-xL, and cyclin D1. Additionally, normal and cancerous colon cell lines, as well as the normal colon of mice, are all affected by GPR109A/butyrate'ssuppressionof nuclear factor-kappaB activation. These studies demonstrate that the colonic butyrate-induced tumor-suppressive effects are mediated by GPR109A.

GPR109A related products

Structure Cat No. Product Name CAS No. Product Description
V4315 MK-0354 851776-28-8 MK-0354 is a novel and potent partial agonist of GPR109a receptor for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
V4313 MK-6892 917910-45-3 MK-6892 (MK6892) is a novel, potent and selective full agonist for GPR109A, which is a high affinity nicotinic acid receptor.
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