Pyruvate Dehydrogenase Kinases: Therapeutic Targets for Diabetes and Cancers [PDF]
Diabetes & Metabolism Journal, 2015 Impaired glucose homeostasis is one of the risk factors for causing metabolic diseases including obesity, type 2 diabetes, and cancers. In glucose metabolism, pyruvate dehydrogenase complex (PDC) mediates a major regulatory step, an irreversible reaction
Nam Ho Jeoung
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Dichloroacetate, a pyruvate dehydrogenase kinase inhibitor, ameliorates type 2 diabetes via reduced gluconeogenesis [PDF]
Heliyon, 2022 Aims: Pyruvate dehydrogenase (PDH) catalyzes the decarboxylation of pyruvate to acetyl-CoA, which plays a key role in linking cytosolic glycolysis to mitochondria metabolism.
Yuko Katayama +3 more
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Pyruvate dehydrogenase kinase supports macrophage NLRP3 inflammasome activation during acute inflammation [PDF]
Cell Reports, 2023 Summary: Activating the macrophage NLRP3 inflammasome can promote excessive inflammation with severe cell and tissue damage and organ dysfunction.
Allison K. Meyers +17 more
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Transcriptional Regulation of Pyruvate Dehydrogenase Kinase [PDF]
Diabetes & Metabolism Journal, 2012 The pyruvate dehydrogenase complex (PDC) activity is crucial to maintains blood glucose and ATP levels, which largely depends on the phosphorylation status by pyruvate dehydrogenase kinase (PDK) isoenzymes.
Ji Yun Jeong +3 more
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The Role of Pyruvate Dehydrogenase Kinase in Diabetes and Obesity [PDF]
Diabetes & Metabolism Journal, 2014 The pyruvate dehydrogenase complex (PDC) is an emerging target for the treatment of metabolic syndrome. To maintain a steady-state concentration of adenosine triphosphate during the feed-fast cycle, cells require efficient utilization of fatty acid and ...
In-Kyu Lee
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Pyruvate Dehydrogenase Kinase 1 inhibition mediated oxidative phosphorylation enhancement in cartilage promotes osteoarthritis progression [PDF]
BMC Musculoskeletal Disorders, 2023 Osteoarthritis (OA) is a common disease characterized by cartilage degradation. Growing evidence showed that glucose metabolism impacts joint homeostasis and an imbalance between glycolysis and oxidative phosphorylation (OXPHOS) may exacerbate OA ...
Xian Yang +8 more
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Pyruvate dehydrogenase kinases (PDKs): an overview toward clinical applications [PDF]
Bioscience Reports, 2021 Abstract Pyruvate dehydrogenase kinase (PDK) can regulate the catalytic activity of pyruvate decarboxylation oxidation via the mitochondrial pyruvate dehydrogenase complex, and it further links glycolysis with the tricarboxylic acid cycle and ATP generation.
Xiuxiu Wang +3 more
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Development of a cell-based target engagement assay for pyruvate dehydrogenase kinase [PDF]
SLAS DiscoveryPyruvate dehydrogenase kinases (PDHKs) are non-canonical serine/threonine kinases that regulate the pyruvate dehydrogenase complex. Given their central role in metabolism, dysregulation of PDHKs has been linked with a broad variety of pathological ...
Mya D. Gough +5 more
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Bovine heart pyruvate dehydrogenase kinase stimulation by monovalent ions
Journal of Biological Chemistry, 1989 The effects of monovalent ions on endogenous pyruvate dehydrogenase (PDH) kinase activity in purified bovine heart pyruvate dehydrogenase complex were investigated. Activity of PDH kinase was stimulated 1.9-, 1.95-, 1.65-, and 1.4-fold by 10 mM K+, Rb+, NH+4, and Cs+, respectively, whereas Na+ and Li+ had no effect on PDH kinase activity.
John Robertson +2 more
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Histidine mutagenesis of Arabidopsis thaliana pyruvate dehydrogenase kinase [PDF]
European Journal of Biochemistry, 2002 Pyruvate dehydrogenase kinase (PDK) is the primary regulator of flux through the mitochondrial pyruvate dehydrogenase complex (PDC). Analysis of the primary amino‐acid sequences of PDK from various sources reveals that these enzymes include the five domains characteristic of prokaryotic two‐component His‐kinases, despite the fact that PDK exclusively ...
Alejandro Tovar‐Méndez +2 more
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