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.
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- C5675 Fendiline (hydrochloride)中文名: 盐酸芬地林Summary: α2-肾上腺素能受体拮抗剂
- C5518 γ-Linolenic Acid中文名: γ-亚麻酸Summary: 弱LTB4受体拮抗剂
- C5416 REV 5901Summary: 半胱氨酰-白三烯受体的拮抗剂
- C5513 S-2 MethanandamideSummary: 有效的CB1受体激动剂
- C5509 S-1 MethanandamideSummary: CB1受体的配体
- C5580 RaceanisodamineSummary: α1肾上腺素受体的弱拮抗剂
- C5611 VU0483605Summary: mGluR1的选择性正变构调节剂(PAM)
- C5718 ML-031Summary: S1P2的激动剂
- C5324 U-44069Summary: TP受体激动剂