Metabolism
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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A4310 Rosiglitazone HClSummary: PPARγ agonist
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A4311 PF-4981517Summary: CYP3A4 inhibitor,potent and selective
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A4313 Cobicistat (GS-9350)Target: Cytochrome P450 (CYP450)Summary: Selective CYP3A inhibitor
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A4316 KetoconazoleTarget: Cytochrome P450 (CYP450)Summary: Inhibitor of cyclosporine oxidase and testosterone 6 beta-hydroxylase
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A4317 Apremilast (CC-10004)Target: Phosphodiesterases (PDEs)Summary: PDE4 inhibitor
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A4318 AvasimibeTarget: Acyl coenzyme A: cholesterol acyltransferasesSummary: ACAT inhibitor,orally bioavailable
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A4319 RoflumilastSummary: PDE-4 inhibitor
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A4320 VoriconazoleSummary: CYP51 inhibitor
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A4321 Sildenafil CitrateTarget: Phosphodiesterases (PDEs)Summary: Treat erectile dysfunction and PAH
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A4322 ClarithromycinTarget: Cytochrome P450 (CYP450)Summary: CYP3A inhibitor, potent