GPCR/G protein - AdipoR1 - Sigma Receptors - LPA Receptors - Adenosine Deaminases
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.
- B6765 Rimcazole dihydrochlorideTarget: Sigma ReceptorsSummary: σ受体拮抗剂
- B6364 PRE-084 hydrochloride1 CitationTarget: Sigma ReceptorsSummary: σ1受体激动剂
- B7515 1-Oleoyl lysophosphatidic acid sodium saltTarget: LPA ReceptorsSummary: 激活LPA受体
- B1591 Ki16198Target: LPA ReceptorsSummary: LPA拮抗剂
- B1879 AdipoRonTarget: AdipoR1|AdipoR2Summary: AdipoR1/2激动剂
- A1987 Ki164254 CitationTarget: LPA ReceptorsSummary: LPA受体拮抗剂
- A3708 Pentostatin1 Citation中文名: 喷司他丁Target: Adenosine DeaminasesSummary: 腺苷脱氨酶抑制剂
- A3170 AM9662 CitationTarget: LPA ReceptorsSummary: LPA1拮抗剂
- A3167 AM-095 free baseTarget: LPA ReceptorsSummary: 有效的LPA1受体拮抗剂