GPCR/G protein
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.
- C6668 Methylbenactyzine Bromide
- C6665 Higenamine hydrochloride中文名: 盐酸去甲乌头碱
- C6646 Methylene Blue中文名: 亚甲蓝
- C6594 Propantheline bromide中文名: 普鲁本辛;溴丙胺太林;溴丙胺西林
- C6570 Dimenhydrinate中文名: 茶苯海明;乘晕宁
- C6550 Dexamethasone phosphate disodium中文名: 地塞米松磷酸二钠
- C6542 Amitraz中文名: 双甲脒;阿米曲士;阿米曲拉
- C5822 p-iodo-Clonidine (hydrochloride)Summary: α2-肾上腺素能受体的部分激动剂
- C5743 ONO-8130Summary: 口服生物可用的前列腺素E2(PGE2)受体EP拮抗剂
- C5824 GPR120 Compound ASummary: 口服、高亲和力的GPR120激动剂