GPCR/G protein - Glucagon-like peptide 1 (GLP-1) receptors - Insulin and Insulin-like Receptors - Progesterone Receptors - Calcium-Sensing Receptors (CaSRs)
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.
- B7504 R 568 hydrochlorideTarget: Calcium-Sensing Receptors (CaSRs)Summary: 人类钙敏感受体(hCaSR)的正变构调节剂
- B6943 Exendin-3 (9-39) amide1 CitationTarget: Glucagon-like peptide 1 (GLP-1) receptorsSummary: GLP-1受体拮抗剂
- B1511 Mifepristone3 Citation中文名: 美服培酮Target: Progesterone Receptors|Glucocorticoid ReceptorsSummary: 孕激素受体拮抗剂
- A3667 NPS-2143 hydrochlorideTarget: Calcium-Sensing Receptors (CaSRs)Summary: 钙离子敏感受体拮抗剂
- A3608 MK 0893Target: Insulin and Insulin-like Receptors|Glucagon ReceptorsSummary: 胰高血糖素受体/ IGF-1R拮抗剂
- A3408 Exendin-4中文名: 艾塞那肽Target: Glucagon-like peptide 1 (GLP-1) receptorsSummary: GLP-1激活剂