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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A3358 DeltarasinTarget: Phosphodiesterases (PDEs)Summary: KRAS-PDEδ interaction inhibitor
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A3493 INCB024360 analogueSummary: potent and selective inhibitor of IDO1
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A8202 Abiraterone acetateTarget: Cytochrome P450 (CYP450)Summary: Cytochrome p450 17a1 inhibitor
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A4300 GW96621 CitationSummary: PPARγ antagonist
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A4316 KetoconazoleTarget: Cytochrome P450 (CYP450)Summary: Inhibitor of cyclosporine oxidase and testosterone 6 beta-hydroxylase
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A4330 IsotretinoinTarget: RARsSummary: Dopamine β-hydroxylase activator
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A4333 CPI-6131 CitationTarget: Pyruvate dehydrogenases (PDH)Summary: PDH/α-KGDH inhibitor
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A4346 AminophyllineTarget: Phosphodiesterases (PDEs)Summary: Pan-PDE inhibitor
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A4347 Methotrexate2 CitationTarget: Folate AnalogueSummary: Folate antagonist,inhibits DFHR
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A4355 Tosedostat (CHR2797)1 CitationTarget: AminopeptidasesSummary: Aminopeptidase inhibitor