Pyruvate Dehydrogenase Kinases: Therapeutic Targets for Diabetes and Cancers [PDF]
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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Pyruvate dehydrogenase (PDH) catalyzes the conversion of pyruvate to acetyl-coenzyme A, which enters into the Krebs cycle, providing adenosine triphosphate (ATP) to the cell.
Michael I. Koukourakis+4 more
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Transcriptional Regulation of Pyruvate Dehydrogenase Kinase [PDF]
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]
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]
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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Monovalent Cation Activation of Plant Pyruvate Dehydrogenase Kinase [PDF]
The pyruvate dehydrogenase kinase-catalyzed inactivation of the pyruvate dehydrogenase complex was studied using dialyzed, soluble proteins from mitochondria purified from green leaf tissue of Pisum sativum L. seedlings. At subsaturating ATP concentrations, K+ or NH4+, but not Na+, stimulated the pyruvate dehydrogenase kinase by lowering the Km(ATP ...
Kathryn A. Schuller+2 more
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Dichloroacetate, a pyruvate dehydrogenase kinase inhibitor, ameliorates type 2 diabetes via reduced gluconeogenesis [PDF]
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 as a Novel Therapeutic Target in Oncology [PDF]
Current drug development in oncology is non-selective as it typically focuses on pathways essential for the survival of all dividing cells. The unique metabolic profile of cancer, which is characterized by increased glycolysis and suppressed ...
Gopinath eSutendra+1 more
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The pivotal role of pyruvate dehydrogenase kinases in metabolic flexibility [PDF]
Metabolic flexibility is the capacity of a system to adjust fuel (primarily glucose and fatty acids) oxidation based on nutrient availability. The ability to alter substrate oxidation in response to nutritional state depends on the genetically influenced balance between oxidation and storage capacities.
Shuai Zhang+4 more
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Pyruvate dehydrogenase kinase supports macrophage NLRP3 inflammasome activation during acute inflammation [PDF]
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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