AMPK
AMPK (5' AMP-activated protein kinase) is an enzyme that plays a role in cellular energy homeostasis. It consists of three proteins (subunits) that together make a functional enzyme, conserved from yeast to humans. The heterotrimeric protein AMPK is formed by α, β, and γ subunits. Each of these three subunits takes on a specific role in both the stability and activity of AMPK. It is expressed in a number of tissues, including the liver, brain, and skeletal muscle. The net effect of AMPK activation is stimulation of hepatic fatty acid oxidation, ketogenesis, stimulation of skeletal muscle fatty acid oxidation and glucose uptake, inhibition of cholesterol synthesis, lipogenesis, and triglyceride synthesis, inhibition of adipocyte lipolysis and lipogenesis, and modulation of insulin secretion by pancreatic beta-cells. It should not be confused with cyclic AMP-activated protein kinase (protein kinase A).
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PT 1是AMPK 激动剂。
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Phenformin盐酸盐具有抗糖尿病和抗癌活性。
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Dorsomorphin是AMPK选择性抑制剂，Ki为109 nM，还能抑制ALK2，ALK3和ALK6。
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Dorsomorphin 2HCl是一种有效的，可逆的AMPK选择性抑制剂，Ki为109 nM，对ZAPK， SYK， PKCθ， PKA和JAK3没有显著的抑制作用。
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A-769662是一种可逆的AMPK激活剂，EC50为0.8 μM，对GPPase/FBPase活性几乎没有作用效果。
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