The pyruvate dehydrogenase complex in cancer: An old metabolic gatekeeper regulated by new pathways and pharmacological agents

Metabolic modulation of cancer: a new frontier with great translational potential

(2015) Adam Kinnaird et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells

(2015) Jonathan D. Moore et al.   Oncotarget

Mito-DCA: A Mitochondria Targeted Molecular Scaffold for Efficacious Delivery of Metabolic Modulator Dichloroacetate

(2014) Rakesh K. Pathak et al.   ACS Chemical Biology

A Nuclear Pyruvate Dehydrogenase Complex Is Important for the Generation of Acetyl-CoA and Histone Acetylation

(2014) Gopinath Sutendra et al.   CELL

SIRT3 deacetylates and increases pyruvate dehydrogenase activity in cancer cells

(2014) Ozkan Ozden et al.   FREE RADICAL BIOLOGY AND MEDICINE

Tyr-301 Phosphorylation Inhibits Pyruvate Dehydrogenase by Blocking Substrate Binding and Promotes the Warburg Effect

(2014) Jun Fan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Tyr-94 Phosphorylation Inhibits Pyruvate Dehydrogenase Phosphatase 1 and Promotes Tumor Growth

(2014) Changliang Shan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery and Optimization of 4,5-Diarylisoxazoles as Potent Dual Inhibitors of Pyruvate Dehydrogenase Kinase and Heat Shock Protein 90

(2014) Tao Meng et al.   JOURNAL OF MEDICINAL CHEMISTRY

Comprehensive review on lactate metabolism in human health

(2014) M. Adeva-Andany et al.   MITOCHONDRION

Tyr Phosphorylation of PDP1 Toggles Recruitment between ACAT1 and SIRT3 to Regulate the Pyruvate Dehydrogenase Complex

(2014) Jun Fan et al.   MOLECULAR CELL

Influence of Metabolism on Epigenetics and Disease

(2013) William G. Kaelin et al.   CELL

Structure-guided Development of Specific Pyruvate Dehydrogenase Kinase Inhibitors Targeting the ATP-binding Pocket

(2013) Shih-Chia Tso et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

SIRT5-Mediated Lysine Desuccinylation Impacts Diverse Metabolic Pathways

(2013) Jeongsoon Park et al.   MOLECULAR CELL

A key role for mitochondrial gatekeeper pyruvate dehydrogenase in oncogene-induced senescence

(2013) Joanna Kaplon et al.   NATURE

Phenylbutyrate Therapy for Pyruvate Dehydrogenase Complex Deficiency and Lactic Acidosis

(2013) R. Ferriero et al.   Science Translational Medicine

Clinical and Experimental Applications of Sodium Phenylbutyrate

(2013) Tommaso Iannitti et al.   Drugs in research & development

Activating oxidative phosphorylation by a pyruvate dehydrogenase kinase inhibitor overcomes sorafenib resistance of hepatocellular carcinoma

(2012) Y-C Shen et al.   BRITISH JOURNAL OF CANCER

Metabolic Regulation of Epigenetics

(2012) Chao Lu et al.   Cell Metabolism

Glucose Oxidation Modulates Anoikis and Tumor Metastasis

(2012) S. Kamarajugadda et al.   MOLECULAR AND CELLULAR BIOLOGY

Mitochondrial activation by inhibition of PDKII suppresses HIF1a signaling and angiogenesis in cancer

(2012) G Sutendra et al.   ONCOGENE

Overexpression of Pyruvate Dehydrogenase Kinase 3 Increases Drug Resistance and Early Recurrence in Colon Cancer

(2011) Chun-Wun Lu et al.   AMERICAN JOURNAL OF PATHOLOGY

p53 Negatively Regulates Transcription of the Pyruvate Dehydrogenase Kinase Pdk2

(2011) T. Contractor et al.   CANCER RESEARCH

Erk regulation of pyruvate dehydrogenase flux through PDK4 modulates cell proliferation

(2011) A. R. Grassian et al.   GENES & DEVELOPMENT

Non-redox-active lipoate derivates disrupt cancer cell mitochondrial metabolism and are potent anticancer agents in vivo

(2011) Zuzana Zachar et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Tyrosine Phosphorylation of Mitochondrial Pyruvate Dehydrogenase Kinase 1 Is Important for Cancer Metabolism

(2011) Taro Hitosugi et al.   MOLECULAR CELL

Anticancer drugs that target metabolism: Is dichloroacetate the new paradigm?

(2010) Ioanna Papandreou et al.   INTERNATIONAL JOURNAL OF CANCER

Butyrate elicits a metabolic switch in human colon cancer cells by targeting the pyruvate dehydrogenase complex

(2010) Jean-Marc Blouin et al.   INTERNATIONAL JOURNAL OF CANCER

Reversal of the glycolytic phenotype by dichloroacetate inhibits metastatic breast cancer cell growth in vitro and in vivo

(2009) Ramon C. Sun et al.   BREAST CANCER RESEARCH AND TREATMENT

Mitaplatin, a potent fusion of cisplatin and the orphan drug dichloroacetate

(2009) Shanta Dhar et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

(2009) M. G. Vander Heiden et al.   SCIENCE

ATP-Citrate Lyase Links Cellular Metabolism to Histone Acetylation

(2009) K. E. Wellen et al.   SCIENCE

Role of dichloroacetate in the treatment of genetic mitochondrial diseases☆

(2008) Peter W. Stacpoole et al.   ADVANCED DRUG DELIVERY REVIEWS

Dichloroacetate (DCA) as a potential metabolic-targeting therapy for cancer

(2008) E D Michelakis et al.   BRITISH JOURNAL OF CANCER

Pyruvate Dehydrogenase Kinase-4 Structures Reveal a Metastable Open Conformation Fostering Robust Core-free Basal Activity

(2008) R. Max Wynn et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Regulation of the PDK4 Isozyme by the Rb-E2F1 Complex

(2008) Michael C. F. Hsieh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Pyruvate Dehydrogenase Complex Activity Controls Metabolic and Malignant Phenotype in Cancer Cells

(2008) Thomas McFate et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Induction of Pyruvate Dehydrogenase Kinase-3 by Hypoxia-inducible Factor-1 Promotes Metabolic Switch and Drug Resistance

(2008) Chun-Wun Lu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis for Inactivation of the Human Pyruvate Dehydrogenase Complex by Phosphorylation: Role of Disordered Phosphorylation Loops

(2008) Masato Kato et al.   STRUCTURE