Metabolism
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.
- C5719 Oleyl Trifluoromethyl KetoneSummary: 有效的FAAH抑制剂
- C5811 5,8,11-Eicosatriynoic AcidSummary: 非选择性脂氧合酶(12-LO)抑制剂
- C5763 Cycloguanil (hydrochloride)中文名: 环氯胍盐酸盐Summary: 二氢叶酸还原酶(DHFR)抑制剂
- C5678 ST638Summary: 酪氨酸激酶抑制剂和PLD抑制剂
- C5671 RB394Summary: 可溶性环氧化物水解酶(sEH)和PPARγ的双重调节剂
- C5625 ONO-RS-082Summary: Ca2+-依赖性磷脂酶A2的可逆抑制剂
- C5452 Monoacylglycerol Lipase Inhibitor 21Summary: 单酰基甘油脂肪酶(MAGL)和FAAH抑制剂
- C5491 trans-AUCBSummary: 可溶性环氧化物水解酶(sEH)的有效抑制剂
- C5572 SR 2595Summary: PPARγ的反向激动剂
- C5435 G3335Summary: PPARγ拮抗剂