GPCR/G protein - Angiotensin-Converting Enzymes (ACEs) - S1P receptors - prostaglandin FP receptor
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.
- B4575 AL 8810Target: prostaglandin FP receptorSummary: 前列腺素F2α(FP)受体拮抗剂
- B7634 RP 001 hydrochlorideTarget: S1P receptorsSummary: S1P1受体激动剂
- B1214 Perindopril中文名: 培哚普利Target: Angiotensin-Converting Enzymes (ACEs)Summary: ACE抑制剂
- B3225 BAF312 (Siponimod)1 Citation中文名: 辛波莫德Target: S1P receptorsSummary: S1P受体激动剂
- A8548 Fingolimod (FTY720)中文名: 盐酸芬戈莫德Target: S1P receptorsSummary: S1P受体激动剂