GPCR/G protein
All GPCRs share a common seven trans-membrane structure. GPCRs are associated with heterotrimeric G-proteins which are GTP-binding proteins made of alpha, beta, and gamma subunits. When a ligand binds to GPCR, it activates the attached G-protein, the GDP is replaced with GTP. The activated G-protein then dissociates into an alpha and a beta-gamma complex which activates downstream signaling pathways. These intracellular signaling pathways include cAMP/PKA, calcium/NFAT, phospholipase C, protein tyrosine kinases, MAP kinases, PI-3-kinase, nitric oxide/cGMP, Rho, and JAK/STAT.
GPCRs are one of the most important therapeutic targets for various diseases, over 30% of all modern medicinal drugs target this family. Aberrant GPCR functions are involved in pathological conditions such as neurological, immunological and hormonal disorders. A large number of GPCRs have been identified, but whose ligands are not known, are classified as orphan receptors.
- B5304 Apelin-36 (rat, mouse)Summary: Endogenous APJ receptor agonist
- B5306 Obestatin (rat)Summary: Endogenous peptide that suppresses food intake and body weight-gain
- B5307 CH 275Summary: Potent somatostatin receptor 1 (sst1) agonist
- B5311 UFP 803Summary: Urotensin-II (UT) receptor ligand
- B5316 CGP 42112Summary: angiotensin AT2 receptor ligand
- B5325 Galanin (1-29) (rat, mouse)Summary: Non-selective galanin receptor agonist
- B5326 M617Summary: Selective galanin GAL1 receptor agonist
- B5327 M871Summary: Selective galanin GAL2 receptor antagonist
- B5328 AR-M 1896Summary: Selective GAL2 agonist
- B5329 Bay 55-9837Summary: Selective VPAC2 receptor agonist