GPCR/G protein - Glucagon-like peptide 1 (GLP-1) receptors - Insulin and Insulin-like Receptors - 5-HT1 Receptor - Serotonin reuptake
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.
- B6347 Methylergometrine maleate中文名: 马来酸甲麦角新碱Target: 5-HT1 Receptor|5-HT2 ReceptorSummary: 5-HT1/5-HT2受体拮抗剂
- B6943 Exendin-3 (9-39) amide1 CitationTarget: Glucagon-like peptide 1 (GLP-1) receptorsSummary: GLP-1受体拮抗剂
- B2251 Naratriptan中文名: 盐酸那拉曲坦,盐酸纳拉曲坦Target: 5-HT1 ReceptorSummary: 选择性5-HT1受体亚型激动剂
- B1205 Fluvoxamine中文名: 氟伏沙明Target: Serotonin reuptakeSummary: 选择性5-羟色胺再摄取抑制剂
- A3608 MK 0893Target: Insulin and Insulin-like Receptors|Glucagon ReceptorsSummary: 胰高血糖素受体/ IGF-1R拮抗剂
- A3408 Exendin-4中文名: 艾塞那肽Target: Glucagon-like peptide 1 (GLP-1) receptorsSummary: GLP-1激活剂