GPCR/G protein - DREADD Ligands - CCR - Melatonin 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.
- B6274 N-AcetyltryptamineTarget: Melatonin ReceptorsSummary: 褪黑激素受体调节剂
- A1748 Ramelteon1 Citation中文名: 雷美替胺Target: Melatonin ReceptorsSummary: MT1/MT2激动剂
- A3494 INCB3344Target: CCRSummary: CCR2趋化因子受体拮抗剂
- A3317 Clozapine N-oxide(CNO)1 Citation中文名: 氯氮平的N-氧化物Target: DREADD LigandsSummary: Clozapine代谢产物,用于化学遗传学