Metabolism - Ftase - Phosphodiesterases (PDEs)
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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- B6988 BRL 50481Target: Phosphodiesterases (PDEs)Summary: PDE7抑制剂
- B6304 Etazolate hydrochloride2 CitationTarget: Phosphodiesterases (PDEs)Summary: PDE-4抑制剂和选择性GABA-A受体调节剂
- B3703 LB42708Target: FtaseSummary: FTase (法尼基转移酶) 选择性抑制剂
- B3439 Udenafil中文名: 乌地那非Target: Phosphodiesterases (PDEs)Summary: PDE5抑制剂
- B1386 Milrinone中文名: 米力农Target: Phosphodiesterases (PDEs)Summary: PDE3抑制剂
- B2276 Vinpocetine中文名: 长春西汀Target: Phosphodiesterases (PDEs)Summary: PDE抑制剂
- A3358 DeltarasinTarget: Phosphodiesterases (PDEs)Summary: KRAS-PDEδ相互作用抑制剂
- A4346 Aminophylline中文名: 氨茶碱,氨基非林Target: Phosphodiesterases (PDEs)Summary: Pan-PDE抑制剂
- A4340 Pimobendan中文名: 匹莫苯丹,匹莫苯Target: Phosphodiesterases (PDEs)Summary: PDE3抑制剂和Ca2+通道敏化剂
- A4334 Avanafil中文名: 阿伐那非Target: Phosphodiesterases (PDEs)Summary: PDE5抑制剂