GPCR/G protein - Na /Ca2 Exchangers (NCXs) - CXCR - 5-HT2 Receptor - 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.
- 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
- B1465 Plerixafor 8HCl (AMD3100 8HCl)中文名: 普乐沙福八盐酸盐Target: CXCRSummary: CXCR4拮抗剂
- A3811 SEA04004 CitationTarget: Na /Ca2 Exchangers (NCXs)Summary: 特异性的Na+/Ca2+交换抑制剂
- A3803 SCH 563705Target: CXCRSummary: CXCR2/CXCR1拮抗剂
- A3802 SCH 5271235 CitationTarget: CXCRSummary: CXCR1和CXCR2拮抗剂
- A3752 Reparixin1 Citation中文名: 瑞帕利辛Target: CXCRSummary: CXCL8受体和CXCR1/CXCR2活化的抑制剂