GPCR/G protein - adrenoceptor - 5-HT2 Receptor - Adenosine Kinases - Free Fatty Acid Receptors
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.
- B7792 AH 76141 CitationTarget: Free Fatty Acid ReceptorsSummary: FFA4/GPR120拮抗剂
- B6552 CGP 20712 dihydrochlorideTarget: adrenoceptorSummary: β1拮抗剂
- B6347 Methylergometrine maleate中文名: 马来酸甲麦角新碱Target: 5-HT1 Receptor|5-HT2 ReceptorSummary: 5-HT1/5-HT2受体拮抗剂
- B5298 ABT 702 dihydrochlorideTarget: Adenosine KinasesSummary: 腺苷激酶抑制剂
- A8474 Mirabegron (YM178)中文名: 米拉贝隆Target: adrenoceptorSummary: 选择性β3肾上腺素受体激动剂
- A1709 GW9508Target: Free Fatty Acid ReceptorsSummary: FFA1/GPR40激动剂
- A3895 TUG-770Target: Free Fatty Acid ReceptorsSummary: FFA1/GPR40激动剂
- A3125 5-Iodotubercidin中文名: 5-碘杀结核菌素Target: Adenosine KinasesSummary: 腺苷激酶抑制剂