1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR109A

GPR109A

GPR109A is a G-protein-coupled receptor for nicotinate but recognizes butyrate with low affinity. GPR109A is expressed in the lumen-facing apical membrane of colonic and intestinal epithelial cells and that the receptor recognizes butyrate as a ligand. The expression of GPR109A is silenced in colon cancer in humans, in a mouse model of intestinal/colon cancer, and in colon cancer cell lines. The tumor-associated silencing of GPR109A involves DNA methylation directly or indirectly. Reexpression of GPR109A in colon cancer cells induces apoptosis, but only in the presence of its ligands butyrate and nicotinate. Butyrate is an inhibitor of histone deacetylases, but apoptosis induced by activation of GPR109A with its ligands in colon cancer cells does not involve inhibition of histone deacetylation. The primary changes in this apoptotic process include down-regulation of Bcl-2, Bcl-xL, and cyclin D1 and up-regulation of death receptor pathway. In addition, GPR109A/butyrate suppresses nuclear factor-kappaB activation in normal and cancer colon cell lines as well as in normal mouse colon. These studies show that GPR109A mediates the tumor-suppressive effects of the bacterial fermentation product butyrate in colon.

GPR109A 相关产品 (4):

Cat. No. Product Name Effect Purity
  • HY-10680
    MK-6892 Agonist 99.43%
    MK-6892 是一种有效的选择性烟酸 (NA) 受体 GPR109A 激动剂。MK-6892 作用于人 GPR109A 的 KiEC50 分别为 4 nM 和 16 nM。
  • HY-13008
    MK-0354 Agonist 98.03%
    MK-0354是特异性的 GPR109a 受体激动剂, 作用于hGPR109a/mGPR109a, EC50分别为1.65 μM 和1.08 μM, 对GPR109b没有作用效果。
  • HY-103252
    Monomethyl fumarate Agonist
    Monomethyl fumarate 是 Dimethyl fumarate (DMF) 的活性代谢产物,一种有效的 GPR109A 激动剂。Monomethyl fumarate 具有用于多种神经保护途径和其他视网膜疾病模型的潜力。
  • HY-119222
    GSK256073 Agonist
    GSK256073 是一种有效的、选择性的、口服活性的 GPR109A 激动剂,是一种持久的 HCA2 激动剂,其 pEC50 为 7.5 (Human HCA2)。GSK256073 可通过抑制脂降解而明显改善葡萄糖稳态,具有研究 2 型糖尿病 (T2DM) 和血脂异常的潜力。
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