GPCR/G protein
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.
- C5386 N-Acetylserotonin中文名: N-乙酰血清素,N-乙酰基-5-羟色胺Summary: 褪黑素受体MT1、MT2和MT3的激动剂
- C5367 6-OAUSummary: GPR84的合成激动剂
- C5331 O-Phospho-D-SerineSummary: 代谢型谷氨酸受体mGluR4的弱激动剂
- C5329 Calindol (hydrochloride)Summary: 钙敏感受体(CaSR)的激活剂
- C5286 (R,S)-Atenolol中文名: 阿替洛尔Summary: β1-肾上腺素能受体拮抗剂
- C5282 Adenosine Kinase Inhibitor (hydrate)Summary: 腺苷激酶抑制剂
- C5311 NESS 0327Summary: 强效的大麻素(CB)受体拮抗剂
- C5552 Tetrahydromagnolol中文名: 四氢厚朴酚Summary: 外周CB2受体激动剂
- C5389 (±)trans-2,5-bis-(3,4,5-Trimethoxyphenyl)-1,3-dioxolaneSummary: PAF受体拮抗剂
- C5385 Butenoyl PAFSummary: PAF受体激动剂