GPCR G2A/GPR132 agonist
CAS：233691-67-3
分子式：C23H31N3O6
分子量：445.51
纯度：98%
存储：Store at -20°C

Background:

Commendamide (N-acyl-3-hydroxypalmitoyl-glycine) is a newly discovered GPCR G2A/GPR132 agonist (EC50=11.8 μM) that isolated from Bacteroides vulgatus. [1]

G2A/GPR132 belongs to the guanine nucleotide-binding protein (G protein)-coupled receptor (GPCR) superfamily. GPR132/G2A is first reported to be a transcriptional target for BCR-ABL tyrosine kinase attenuating B-cell expansion in vitro and arresting cells at G2 during mitosis. It has been involved in autoimmune disease and atherosclerosis. [1]

Commendamide and structurally related endogenous long-chain N-Acyl-amides activates discrete human receptors. In a screen for agonist activity against a library of 242 GPCRs, commendamide is found to activate a single receptor G2A/GPR132. This activity is confirmed by a synthetic sample of commendamide. Commendamide analogs with changes in the head group or acyl chain also exhibited reduced GPR132/G2A activity. [1]

Reference:
1. Cohen LJ, Kang HS, Chu J et al. Functional metagenomic discovery of bacterial effectors in the human microbiome and isolation of commendamide, a GPCR G2A/132 agonist. Proc Natl Acad
Sci U S A. 2015 Sep 1;112(35):E4825-34.