GPCR/G protein - Prostate Cancer - Cancer
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.
- B3587 kobe2602Summary: Ras抑制剂
- B1986 NedaplatinSummary: DNA合成抑制剂
- B1591 Ki16198Target: LPA ReceptorsSummary: LPA拮抗剂
- B2231 Amitriptyline HCl中文名: 盐酸阿米替林Target: Trk Receptors|5-HT2 Receptors|Norepinephrine transporter|5-HT TransportersSummary: 血清素/去甲肾上腺素受体/5-HT4/5-HT2抑制剂
- B1214 Perindopril中文名: 培哚普利Target: Angiotensin-Converting Enzymes (ACEs)Summary: ACE抑制剂
- B1465 Plerixafor 8HCl (AMD3100 8HCl)中文名: 普乐沙福八盐酸盐Target: CXCRSummary: CXCR4拮抗剂
- B1466 WZ811Target: CXCRSummary: 高效的CXCR4竞争性拮抗剂
- B2240 Olanzapine中文名: 奥氮平Target: 5-HT2 Receptors|D2 ReceptorsSummary: 5-HT2A和多巴胺D2受体的拮抗剂
- B1511 Mifepristone3 Citation中文名: 美服培酮Target: Progesterone Receptors|Glucocorticoid ReceptorsSummary: 孕激素受体拮抗剂
- B2226 SKI IITarget: Sphingosine kinases (SphKs)Summary: 鞘氨醇激酶(SK)抑制剂