GPCR/G protein - Melanoma - Acute Kidney Injury - Liver Cancer - Breast Cancer
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.
- B2236 Desvenlafaxine中文名: 去甲文拉法辛Target: 5-HT Transporters|Norepinephrine transportersSummary: 5-羟色胺(5-HT)和去甲肾上腺素(NE)再摄取抑制剂
- B1465 Plerixafor 8HCl (AMD3100 8HCl)中文名: 普乐沙福八盐酸盐Target: CXCRSummary: CXCR4拮抗剂
- B1511 Mifepristone3 Citation中文名: 美服培酮Target: Progesterone Receptors|Glucocorticoid ReceptorsSummary: 孕激素受体拮抗剂
- A1987 Ki164254 CitationTarget: LPA ReceptorsSummary: LPA受体拮抗剂
- A3753 Reparixin L-lysine salt1 Citation中文名: 瑞帕利辛L-赖氨酸盐Target: CXCRSummary: CXCL8受体CXCR1/CXCR2活化的抑制剂
- A3752 Reparixin1 Citation中文名: 瑞帕利辛Target: CXCRSummary: CXCL8受体和CXCR1/CXCR2活化的抑制剂
- A3723 Phloretin中文名: 根皮素Target: SGLTSummary: 在苹果中发现的二氢查耳酮
- A3170 AM9662 CitationTarget: LPA ReceptorsSummary: LPA1拮抗剂