GPCR/G protein - CCR - 5-HT3 Receptors - CRF1 Receptors - Angiotensin-Converting Enzymes (ACEs)
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.
- B7275 NBI 35965 hydrochlorideTarget: CRF1 ReceptorsSummary: CRF1拮抗剂
- B2241 Ondansetron中文名: 昂丹司琼Target: 5-HT3 ReceptorsSummary: 血清素5-HT3受体拮抗剂
- B2259 VUF 10166Target: 5-HT3 ReceptorsSummary: 5-HT3受体拮抗剂
- B1214 Perindopril中文名: 培哚普利Target: Angiotensin-Converting Enzymes (ACEs)Summary: ACE抑制剂
- B2258 Tropisetron Hydrochloride中文名: 盐酸托烷司琼Target: 5-HT3 ReceptorsSummary: 5-HT3受体拮抗剂
- A1334 Mosapride Citrate中文名: 莫沙必利柠檬酸盐Target: 5-HT3 Receptors|5-HT4 ReceptorsSummary: 5-HT受体激动剂
- A3926 Vortioxetine中文名: 沃替西汀Target: 5-HT1 Receptors|5-HT7 Receptors|5-HT3 Receptors|SERTSummary: 5-HT受体拮抗剂
- A3494 INCB3344Target: CCRSummary: CCR2趋化因子受体拮抗剂