GPCR/G protein - AdipoR1 - GLP-2 receptor - CCR - Sphingosine kinases (SphKs)
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.
- B5282 GLP-2 (rat)Target: GLP-2 receptorSummary: 肠上皮特异性生长因子
- B1879 AdipoRonTarget: AdipoR1|AdipoR2Summary: AdipoR1/2激动剂
- B2226 SKI IITarget: Sphingosine kinases (SphKs)Summary: 鞘氨醇激酶(SK)抑制剂
- A3717 PF-5431 CitationTarget: Sphingosine kinases (SphKs)Summary: SphK1选择性抑制剂
- A3494 INCB3344Target: CCRSummary: CCR2趋化因子受体拮抗剂