GPCR/G protein - Selective - Sphingosine kinases (SphKs) - Serotonin (5-HT) reuptake - adrenoceptor
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.
- B6552 CGP 20712 dihydrochlorideTarget: adrenoceptorSummary: β1拮抗剂
- 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
- A2436 Fluoxetine HCl中文名: 盐酸氟西汀Target: Serotonin (5-HT) reuptakeSummary: 5-羟色胺重吸收抑制剂
- A3717 PF-5431 CitationTarget: Sphingosine kinases (SphKs)Summary: SphK1选择性抑制剂