GPCR/G protein - Glucocorticoid Receptors - adrenoceptor - 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.
- B4953 Methylprednisolone Sodium Succinate中文名: 甲泼尼龙琥珀酸钠Target: Glucocorticoid ReceptorsSummary: 糖皮质激素
- B6552 CGP 20712 dihydrochlorideTarget: adrenoceptorSummary: β1拮抗剂
- 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
- B1926 Dexamethasone acetate中文名: 醋酸地塞米松Target: Glucocorticoid Receptors|interleukin receptorSummary: IL受体调节剂
- B1511 Mifepristone3 Citation中文名: 美服培酮Target: Progesterone Receptors|Glucocorticoid ReceptorsSummary: 孕激素受体拮抗剂
- A8474 Mirabegron (YM178)中文名: 米拉贝隆Target: adrenoceptorSummary: 选择性β3肾上腺素受体激动剂
- A4233 Methylprednisolone中文名: 甲泼尼龙Target: Glucocorticoid ReceptorsSummary: 细胞凋亡诱导剂,GR激动剂