GPCR/G protein - Animal Experiments
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.
- B7818 ONO-7300243Target: LPASummary: LPA1拮抗剂
- B5910 Rolapitant HCl中文名: 罗拉匹坦Target: NK1 ReceptorsSummary: 神经激肽NK1受体拮抗剂
- B5904 Regadenoson1 Citation中文名: 类伽腺苷Target: Adenosine A2A ReceptorsSummary: A2A腺苷受体激动剂
- B4953 Methylprednisolone Sodium Succinate中文名: 甲泼尼龙琥珀酸钠Target: Glucocorticoid ReceptorsSummary: 糖皮质激素
- B8031 MK-571 sodium salt hydrate3 CitationTarget: CysLT1Summary: CysLT1受体拮抗剂
- B7792 AH 76141 CitationTarget: Free Fatty Acid ReceptorsSummary: FFA4/GPR120拮抗剂
- B5612 BAY 60-6583Target: Adenosine A2B ReceptorsSummary: A2B受体的强效激动剂
- B5321 DOI hydrochlorideTarget: 5-HT2 ReceptorsSummary: 脑通透性、混合型5-HT2A/5-HT2C受体激动剂
- B5082 FR 139317Target: endothelin receptorSummary: 选择性ETA内皮素受体拮抗剂
- B7504 R 568 hydrochlorideTarget: Calcium-Sensing Receptors (CaSRs)Summary: 人类钙敏感受体(hCaSR)的正变构调节剂