Human beta2AR-GPR75-BRIL full length protein-synthetic nanodisc

GPR75 is a member of the G protein-coupled receptor family and is a novel target for the clinical treatment of obesity. Human GPR75 haploinsufficiency exhibits a striking phenotype of low body fat, and GPR75 knockout mice are hypophagic and thin, improving glucose tolerance and insulin sensitivity. To enhance the expression level of GPR75, twenty-four amino acids from the beta2AR receptor (MGQPGNGSAFLLAPNRSHAPDHDV) were used to replace the original residues1-31 in a modified version of the GPR75 receptor. Furthermore, the BRIL sequence was used to replace the original ICL3 loop (237-306) to enhance receptor stability. BRIL is thermostabilized apocytochrome b562 with mutations M7W, H102I, R106L, PDB ID 1M6T.. Human beta2AR-GPR75-BRIL full length protein-synthetic nanodisc. Protein function: G protein-coupled receptor that is activated by the chemokine CCL5/RANTES. Probably coupled to heterotrimeric Gq proteins, it stimulates inositol trisphosphate production and calcium mobilization upon activation. Together with CCL5/RANTES, may play a role in neuron survival through activation of a downstream signaling pathway involving the PI3, Akt and MAP kinases. CCL5/RANTES may also regulate insulin secretion by pancreatic islet cells through activation of this receptor. [The UniProt Consortium]