ArticleThe Journal of biological chemistry2018
A novel inhibitor of pyruvate dehydrogenase kinase stimulates myocardial carbohydrate oxidation in diet-induced obesity.
Article in The Journal of biological chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 33 citations in OpenAlex.
- Small-molecule PS10 inhibits PRRSV replication by targeting HSP90 and multiple viral non-structural proteins.Journal of virology · 2026Article
- Pyruvate dehydrogenase kinases: key regulators of cellular metabolism and therapeutic targets for metabolic diseases.Journal of physiology and biochemistry · 2025Review
- Post-translational modifications of pyruvate dehydrogenase complex in cardiovascular disease.iScience · 2024Review
- Metabolic inflexibility promotes mitochondrial health during liver regeneration.Science (New York, N.Y.) · 2024Article
- Mini Review: the non-neuronal cardiac cholinergic system in type-2 diabetes mellitus.Frontiers in cardiovascular medicine · 2024Review
- Analysis and modification of central carbon metabolism inFrontiers in microbiology · 2023Article
- Pyruvate Dehydrogenase Complex and Glucose Oxidation as a Therapeutic Target in Diabetic Heart Disease.Journal of lipid and atherosclerosis · 2023Review
- A Missense Variant inBiomedicines · 2022Article
- Sepsis, pyruvate, and mitochondria energy supply chain shortage.Journal of leukocyte biology · 2022Review
- Inhibition of pyruvate dehydrogenase kinase improves carbohydrate utilization in Nile tilapia by regulating PDK2/4-PDHE1α axis and insulin sensitivity.Animal nutrition (Zhongguo xu mu shou yi xue hui) · 2022Article
- Altered glycolysis triggers impaired mitochondrial metabolism and mTORC1 activation in diabetic β-cells.Nature communications · 2022Article
- Mechanisms of Myocardial Damage Due to Hyperlipidemia: A Review of Recent Studies.Medical science monitor : international medical journal of experimental and clinical research · 2022Review
- Methodological Developments for Metabolic NMR Spectroscopy from Cultured Cells to Tissue Extracts: Achievements, Progress and Pitfalls.Molecules (Basel, Switzerland) · 2022Review
- PDK4 Inhibition Ameliorates Melatonin Therapy by Modulating Cerebral Metabolism and Remyelination in an EAE Demyelinating Mouse Model of Multiple Sclerosis.Frontiers in immunology · 2022Article
- Acetate rescues defective brain-adipose metabolic network in obese Wistar rats by modulation of peroxisome proliferator-activated receptor-γ.Scientific reports · 2021Article
- Analysis of lncRNA-miRNA-mRNA expression pattern in heart tissue after total body radiation in a mouse model.Journal of translational medicine · 2021Article
- NADPH and Glutathione Redox Link TCA Cycle Activity to Endoplasmic Reticulum Homeostasis.iScience · 2020Article
- Metabolic requirements of Besnoitia besnoiti tachyzoite-triggered NETosis.Parasitology research · 2020Article
- Changes in Myocardial Metabolism Preceding Sudden Cardiac Death.Frontiers in physiology · 2020Review
- Review
Corrections and comments
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Authors and funding
13 authors at 5 institutions in 2 countries.
Funding
Abstract
The pyruvate dehydrogenase complex (PDC) is a key control point of energy metabolism and is subject to regulation by multiple mechanisms, including posttranslational phosphorylation by pyruvate dehydrogenase kinase (PDK). Pharmacological modulation of PDC activity could provide a new treatment for diabetic cardiomyopathy, as dysregulated substrate selection is concomitant with decreased heart function. Dichloroacetate (DCA), a classic PDK inhibitor, has been used to treat diabetic cardiomyopathy, but the lack of specificity and side effects of DCA indicate a more specific inhibitor of PDK is needed. This study was designed to determine the effects of a novel and highly selective PDK inhibitor, 2((2,4-dihydroxyphenyl)sulfonyl) isoindoline-4,6-diol (designated PS10), on pyruvate oxidation in diet-induced obese (DIO) mouse hearts compared with DCA-treated hearts. Four groups of mice were studied: lean control, DIO, DIO + DCA, and DIO + PS10. Both DCA and PS10 improved glucose tolerance in the intact animal. Pyruvate metabolism was studied in perfused hearts supplied with physiological mixtures of long chain fatty acids, lactate, and pyruvate. Analysis was performed using conventional
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.