GPCR/G protein - Cell 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.
- B1358 Epinephrine Bitartrate中文名: 酒石酸肾上腺素Target: adrenergic receptorSummary: 肾上腺素能受体激动剂
- B2248 Ketanserin中文名: 酮色林Target: 5-HT2 ReceptorsSummary: 特异性5-HT2A受体拮抗剂
- B1343 Phenoxybenzamine HCl中文名: 盐酸酚苄明Summary: 肾上腺素能受体拮抗剂
- B2241 Ondansetron中文名: 昂丹司琼Target: 5-HT3 ReceptorsSummary: 血清素5-HT3受体拮抗剂
- B1348 Salbutamol Sulfate中文名: 硫酸沙丁胺醇Summary: β-2肾上腺素能受体激动剂
- B1357 Dexmedetomidine HCl中文名: 盐酸右美托咪定Summary: 高选择性和有效的α-2肾上腺素受体激动剂
- B1351 Xylazine HCl中文名: 盐酸塞拉嗪Summary: α2肾上腺素受体激动剂
- B2259 VUF 10166Target: 5-HT3 ReceptorsSummary: 5-HT3受体拮抗剂
- B1328 Terbutaline Sulfate中文名: 硫酸特布他林Summary: 选择性β2-肾上腺素能受体激动剂
- B1986 NedaplatinSummary: DNA合成抑制剂