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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- B4876 K-Ras(G12C) inhibitor 12Summary: K-Ras(G12C)别构抑制剂
- C5822 p-iodo-Clonidine (hydrochloride)Summary: α2-肾上腺素能受体的部分激动剂
- C5743 ONO-8130Summary: 口服生物可用的前列腺素E2(PGE2)受体EP拮抗剂
- C5824 GPR120 Compound ASummary: 口服、高亲和力的GPR120激动剂
- C5802 CarazololSummary: 高亲和力、亲脂性、非选择性的β-肾上腺素能受体的配体
- C5675 Fendiline (hydrochloride)Summary: α2-肾上腺素能受体拮抗剂
- C5518 γ-Linolenic AcidSummary: 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