Metabolism - Cancer
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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- B6062 Manumycin A中文名: 手霉素ASummary: 法尼基转移酶抑制剂
- B6036 INCB-024360中文名: 艾卡哚司他Target: IDOSummary: 强效的IDO1抑制剂
- A8721 CBR-58841 CitationTarget: 3-phosphoglycerate dehydrogenaseSummary: PHGDH抑制剂
- B4900 Indoximod (NLG-8189)Summary: 吲哚胺2,3-双加氧酶(IDO)途径抑制剂
- B6988 BRL 50481Target: Phosphodiesterases (PDEs)Summary: PDE7抑制剂
- B3607 A9395721 CitationTarget: Stearoyl-CoA 9-desaturase (SCD-1)Summary: 硬脂酰辅酶A去饱和酶1(SCD1)抑制剂
- B1943 Fenofibrate1 Citation中文名: 非诺贝特Summary: PPARα激动剂
- A8522 Simvastatin (Zocor)中文名: 辛伐他汀Target: HMG-CoA ReductasesSummary: HMGCR(HMG-CoA还原酶)抑制剂
- 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