Metabolism - Pyruvate dehydrogenases (PDH) - 5-alpha Reductases - complex I of the mitochondrial electron transport chain - Factor Xa
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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- B5462 Rotenone中文名: 鱼藤酮Target: complex I of the mitochondrial electron transport chainSummary: 线粒体复合物I电子传递链抑制剂
- A1659 Dutasteride中文名: 度他雄胺Target: 5-alpha ReductasesSummary: 5-alpha-还原酶抑制剂
- A4338 Rivaroxaban中文名: 利伐塞班Target: Factor XaSummary: Xa因子抑制剂
- A4333 CPI-6131 CitationTarget: Pyruvate dehydrogenases (PDH)Summary: PDH/α-KGDH抑制剂