Metabolism - Selective
Glucose metabolism plays a significant role in cell proliferation, growth, survival, and tumorgenesis. Hormones such as insulin regulate the maintenance of glucose homeostasis. Insulin binding to the insulin receptor (IR) activates the insulin receptor substrate (IRS) protein, followed by the activation of PI3K/Akt and Erk1/2 signaling pathways, leads to the translocation of Glut4 vesicles, glucose uptake, cell proliferation and survival. Abnormal insulin signaling is implicated in diabetes, obesity, atherosclerosis and neurodegenerative disease etc.
Serine/threonine kinase AMPK upregulates glucose uptake by promoting the expression and function of glucose transporters. AMPK is activated by increased AMP/ATP ratio, resulting from cellular and environmental stress, e.g. low glucose, heat shock, hypoxia and ischemia. AMPK activation positively modulates signaling transductions that refill ATP levels. Moreover, it also stimulates catabolic processes such as fatty acid oxidation and glycolysis through inhibition of ACC and activation of PFK2. AMPK negatively regulates various proteins which are important to ATP-consuming mechanisms, e.g. mTORC2, glycogen synthase, SREBP-1, and TSC2, causing the downregulation/inhibition of gluconeogenesis and glycogen, lipid and protein synthesis.
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- A8522 Simvastatin (Zocor)中文名: 辛伐他汀Target: HMG-CoA ReductasesSummary: HMGCR(HMG-CoA还原酶)抑制剂
- A8504 Pitavastatin Calcium1 Citation中文名: 匹伐他汀钙Target: HMG-CoA ReductasesSummary: 酶HMGCR抑制剂
- A8333 Canagliflozin1 Citation中文名: 卡格列净Target: SGLTSummary: SGLT2的有效选择性抑制剂
- A8306 MOG (35-55)1 CitationSummary: CNS髓磷脂的微量成分
- A2213 17-DMAG (Alvespimycin) HCl1 Citation中文名: 阿螺旋霉素盐酸盐Target: HSP90Summary: Hsp90抑制剂
- A3493 INCB024360 analogueSummary: 有效的和选择性的IDO1抑制剂
- A3358 DeltarasinTarget: Phosphodiesterases (PDEs)Summary: KRAS-PDEδ相互作用抑制剂
- A3215 AZD7687Target: DGATSummary: 强效的选择性DGAT抑制剂
- A3178 AN-2728中文名: 克立硼罗Summary: PDE4抑制剂,抗炎化合物
- A3146 AGI-6780Target: IDH2Summary: IDH2/R140Q突变抑制剂