Metabolism - Pancreatic Carcinoma - Lymphoma - Leukemia - Lung 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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- B4900 Indoximod (NLG-8189)Summary: 吲哚胺2,3-双加氧酶(IDO)途径抑制剂
- A3358 DeltarasinTarget: Phosphodiesterases (PDEs)Summary: KRAS-PDEδ相互作用抑制剂
- A4381 FK866 (APO866)1 Citation中文名: 达珀利奈Target: NamptSummary: NAMPT抑制剂
- A4347 Methotrexate2 Citation中文名: 甲氨蝶呤Target: Folate AnalogueSummary: 叶酸拮抗剂,抑制DFHR。
- A4330 Isotretinoin中文名: 罗可坦,异维A酸Target: RARsSummary: 多巴胺β-羟化酶激活剂
- A4064 NVP-BEP800Target: HSP90Summary: 全合成的HSP90β口服抑制剂
- A4061 IPI-504 (Retaspimycin hydrochloride)3 Citation中文名: 瑞他霉素盐酸盐Target: HSP90Summary: Hsp90抑制剂