Metabolism - Cytochrome P450 (CYP450) - Glycogen Phosphorylases - CETP
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.
清除全部
- 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
- A8403 CP-91149Target: Glycogen PhosphorylasesSummary: 糖原磷酸化酶选择性抑制剂
- A1718 Posaconazole中文名: 泊沙康唑Target: Cytochrome P450 (CYP450)|sterol demethylaseSummary: 甾醇 C14ɑ去甲基化酶抑制剂
- A3374 Dronedarone中文名: 决奈达隆Target: Cytochrome P450 (CYP450)|sodium channel|adrenergic receptor|potassium channel|calcium channelSummary: CYP3A4和2D6抑制剂
- A4377 Evacetrapib (LY2484595)Target: CETPSummary: 强效的CETP选择性抑制剂
- A4375 Anacetrapib (MK-0859)1 Citation中文名: 安塞曲匹Target: CETPSummary: RhCETP/突变型 CETP(C13S) 抑制剂
- A4322 Clarithromycin中文名: 克拉霉素Target: Cytochrome P450 (CYP450)Summary: CYP3A抑制剂
- A4316 Ketoconazole中文名: 酮康唑Target: Cytochrome P450 (CYP450)Summary: 环孢菌素氧化酶和睾酮6β-羟化酶的抑制剂
- A4313 Cobicistat (GS-9350)中文名: 可比司他Target: Cytochrome P450 (CYP450)Summary: CYP3A的选择性抑制剂
- A8202 Abiraterone acetate中文名: 乙酸阿比特龙酯Target: Cytochrome P450 (CYP450)Summary: 细胞色素p450 17a1抑制剂