GPCR/G protein - Selective
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.
- B1343 Phenoxybenzamine HCl中文名: 盐酸酚苄明Summary: 肾上腺素能受体拮抗剂
- B1357 Dexmedetomidine HCl中文名: 盐酸右美托咪定Summary: 高选择性和有效的α-2肾上腺素受体激动剂
- B1328 Terbutaline Sulfate中文名: 硫酸特布他林Summary: 选择性β2-肾上腺素能受体激动剂
- B1986 NedaplatinSummary: DNA合成抑制剂
- B1591 Ki16198Target: LPA ReceptorsSummary: LPA拮抗剂
- B1428 GW842166XTarget: cannabinoid receptorSummary: 大麻素受体激动剂
- B2236 Desvenlafaxine中文名: 去甲文拉法辛Target: 5-HT Transporters|Norepinephrine transportersSummary: 5-羟色胺(5-HT)和去甲肾上腺素(NE)再摄取抑制剂
- B2231 Amitriptyline HCl中文名: 盐酸阿米替林Target: Trk Receptors|5-HT2 Receptors|Norepinephrine transporter|5-HT TransportersSummary: 血清素/去甲肾上腺素受体/5-HT4/5-HT2抑制剂
- B2096 Fluticasone propionate中文名: 丙酸氟替卡松Target: Glucocorticoid ReceptorsSummary: 高亲和力,选择性糖皮质激素受体激动剂
- B1214 Perindopril中文名: 培哚普利Target: Angiotensin-Converting Enzymes (ACEs)Summary: ACE抑制剂