GPCR/G protein - Type 2 Diabetes
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.
- B5612 BAY 60-6583Target: Adenosine A2B ReceptorsSummary: A2B受体的强效激动剂
- B6766 CL 316243 disodium saltSummary: 鼠选择性的β3肾上腺素受体激动剂
- B1214 Perindopril中文名: 培哚普利Target: Angiotensin-Converting Enzymes (ACEs)Summary: ACE抑制剂
- B2210 Azilsartan中文名: 阿齐沙坦Target: Angiotensin AT1 ReceptorsSummary: 强效血管紧张素II 1型(AT1)受体反向激动剂
- B1429 Rimonabant3 Citation中文名: 利莫那班Target: CB1 Receptors|CB2 ReceptorsSummary: CB1 受体拮抗剂
- A3895 TUG-770Target: Free Fatty Acid ReceptorsSummary: FFA1/GPR40激动剂
- 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