GPCR/G protein - Glucocorticoid Receptors - adrenoceptor - 5-HT1 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.
- 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
- B1477 Lurasidone HCl中文名: 盐酸鲁拉西酮Target: 5-HT2 Receptors|D2 Receptors|5-HT1 Receptors|5-HT7 ReceptorsSummary: 多巴胺D2/5-HT2A/5-HT7/5-HT1A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
- A5294 Sumatriptan Succinate中文名: 舒马普坦琥珀酸盐Target: 5-HT1 ReceptorsSummary: 5-HT1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
- A4233 Methylprednisolone中文名: 甲泼尼龙Target: Glucocorticoid ReceptorsSummary: 细胞凋亡诱导剂,GR激动剂