GPCR/G protein - Sigma Receptors - cannabinoid receptor - LPA - Na /Ca2 Exchangers (NCXs)
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.
- B7818 ONO-7300243Target: LPASummary: LPA1拮抗剂
- B6765 Rimcazole dihydrochlorideTarget: Sigma ReceptorsSummary: σ受体拮抗剂
- B6364 PRE-084 hydrochloride1 CitationTarget: Sigma ReceptorsSummary: σ1受体激动剂
- B1428 GW842166XTarget: cannabinoid receptorSummary: 大麻素受体激动剂
- A3811 SEA04004 CitationTarget: Na /Ca2 Exchangers (NCXs)Summary: 特异性的Na+/Ca2+交换抑制剂