GPCR/G protein - CysLT1 - 5-HT4 Receptors - AdipoR1 - CB2 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.
- B8031 MK-571 sodium salt hydrate3 CitationTarget: CysLT1Summary: CysLT1受体拮抗剂
- B1879 AdipoRonTarget: AdipoR1|AdipoR2Summary: AdipoR1/2激动剂
- B1425 BML-190中文名: 吲哚美辛吗啉代酰胺Target: CB2 ReceptorsSummary: CB2受体的配体
- B1429 Rimonabant3 Citation中文名: 利莫那班Target: CB1 Receptors|CB2 ReceptorsSummary: CB1 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