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Overview
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Background
Target: GPR35 IC50: N/ATCS3035, a GPR35 agonist, shows significantly high potency at rat and human GPR35 orthologs with pEC50 values of 5.13 and 5.86, respectively [1]. G protein-coupled receptors (GPCRs) are the largest and most studied group of transmembrane polypeptides. GPR35 is a poorly characterized G protein-coupled receptor that plays an important role in immune-modulation, gastric function and the regulation of insulin secretion. GPR35 is predominantly expressed in the gastro-intestinal tract and immune tissues. The tryptophan metabolite kynurenic acid has been suggested to be the endogenous ligand for GPR35 [1].In vitro: Mutation to alanine of the conserved arginine at position 3.36 in either FLAG-hGPR35-eYFP or FLAG-rGPR35-eYFP resulted in a complete loss of agonist function of TCS3035 [1]. In addition, TCS3035-induced internalization of GPR35 is correlated with TCS3035 potency in receptor-β-arrestin-2 interaction BRET assays. Mutation to alanine of tyrosine 3.32 in transmembrane domain III abolished β-arrestin-2 recruitment in response to TCS3035 [1].In vivo: N/A
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