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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- A8703 IsosafroleTarget: Lactate Dehydrogenases (LDH)Summary: stiripentol类似物,有效的LDH抑制剂。
- B6036 INCB-024360中文名: 艾卡哚司他Target: IDOSummary: 强效的IDO1抑制剂
- A8723 GSK180Target: Kynurenine-3-monooxygenaseSummary: 犬尿氨酸-3-单加氧酶(KMO)抑制剂
- A8721 CBR-58841 CitationTarget: 3-phosphoglycerate dehydrogenaseSummary: PHGDH抑制剂
- B5963 7-Ethoxyresorufin中文名: 乙氧基试卤灵,7-乙氧基-3H-吩恶嗪-3-酮Target: Cytochrome P450 (CYP450)Summary: CYP1A特异性底物
- B4929 GSK 2837808ATarget: Lactate Dehydrogenases (LDH)Summary: 乳酸脱氢酶A(LDHA)抑制剂
- B4900 Indoximod (NLG-8189)Summary: 吲哚胺2,3-双加氧酶(IDO)途径抑制剂
- B7794 BMS 3094032 CitationTarget: Fatty-acid-binding proteins (FABPs)Summary: FABP4抑制剂
- B5508 Alda 1Target: Aldehyde DehydrogenasesSummary: ALDH2激活剂
- B6988 BRL 50481Target: Phosphodiesterases (PDEs)Summary: PDE7抑制剂