Any feedback?
Please rate this page
(enzyme.php)
(0/150)

BRENDA support

Disease on EC 2.7.11.2 - [pyruvate dehydrogenase (acetyl-transferring)] kinase

Please use the Disease Search for a specific query.
Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
DISEASE
TITLE OF PUBLICATION
LINK TO PUBMED
Acidosis
Dichloroacetate attenuates myocardial acidosis and metabolic changes induced by partial occlusion of the coronary artery in dogs.
Acidosis, Lactic
A Mechanism-Based Pharmacokinetic Enzyme Turnover Model for Dichloroacetic Acid Autoinhibition in Rats.
Dichloroacetate enhances apoptotic cell death via oxidative damage and attenuates lactate production in metformin-treated breast cancer cells.
Repurposing phenformin for the targeting of glioma stem cells and the treatment of glioblastoma.
Acute Kidney Injury
Pyruvate dehydrogenase kinase 4 deficiency attenuates cisplatin-induced acute kidney injury.
Adenocarcinoma
p,p'-Dichlorodiphenyltrichloroethane promotes aerobic glycolysis via reactive oxygen species-mediated extracellular signal-regulated kinase/M2 isoform of pyruvate kinase (PKM2) signaling in colorectal cancer cells.
Treatment of Pancreatic Cancer Patient-Derived Xenograft Panel with Metabolic Inhibitors Reveals Efficacy of Phenformin.
Adenocarcinoma of Lung
PDK2 induces Cisplatin-resistance in lung adenocarcinoma via transcriptional regulation of CNNM3.
Adenoma
Isolation of expressed sequence tags of skeletal muscle of neonatal healthy and splay leg piglets and mapping by somatic cell hybrid analysis.
Arrhythmogenic Right Ventricular Dysplasia
A review of the underlying genetics and emerging therapies for canine cardiomyopathies.
Arthritis, Rheumatoid
Synovial fibroblast-derived exosomal microRNA-106b suppresses chondrocyte proliferation and migration in rheumatoid arthritis via down-regulation of PDK4.
Atherosclerosis
Advanced glycation end products enhance macrophage polarization to the M1 phenotype via the HIF-1?/PDK4 pathway.
Pyruvate Dehydrogenase Kinase 4 Promotes Vascular Calcification via SMAD1/5/8 Phosphorylation.
Breast Neoplasms
3D Growth of Cancer Cells Elicits Sensitivity to Kinase Inhibitors but Not Lipid Metabolism Modifiers.
Kisspeptin 10 inhibits the Warburg effect in breast cancer through the Smad signaling pathway: both in vitro and in vivo.
Neuromedin U alters bioenergetics and expands the cancer stem cell phenotype in HER2-positive breast cancer.
P-cadherin induces anoikis-resistance of matrix-detached breast cancer cells by promoting pentose phosphate pathway and decreasing oxidative stress.
Carcinogenesis
Loss of PDK4 expression promotes proliferation, tumorigenicity, motility and invasion of hepatocellular carcinoma cells.
Overexpression of PDK4 is associated with cell proliferation, drug resistance and poor prognosis in ovarian cancer.
Carcinoma
Increased Expression of PDK4 Was Displayed in Gastric Cancer and Exhibited an Association With Glucose Metabolism.
Lung Cancer: A Comparative Study of Metabolism Related Protein Expression in Cancer Cells and Tumor Associated Stroma.
Metabolic Modulation of Clear-cell Renal Cell Carcinoma with Dichloroacetate, an Inhibitor of Pyruvate Dehydrogenase Kinase.
Superior anti-tumor efficacy of diisopropylamine dichloroacetate compared with dichloroacetate in a subcutaneous transplantation breast tumor model.
Carcinoma, Hepatocellular
Activating oxidative phosphorylation by a pyruvate dehydrogenase kinase inhibitor overcomes sorafenib resistance of hepatocellular carcinoma.
Active pyruvate dehydrogenase and impaired gluconeogenesis in orthotopic hepatomas of rats.
Loss of PDK4 expression promotes proliferation, tumorigenicity, motility and invasion of hepatocellular carcinoma cells.
Targeting aerobic glycolysis by dichloroacetate improves Newcastle disease virus-mediated viro-immunotherapy in hepatocellular carcinoma.
Carcinoma, Non-Small-Cell Lung
Blocking Aerobic Glycolysis by Targeting Pyruvate Dehydrogenase Kinase in Combination with EGFR TKI and Ionizing Radiation Increases Therapeutic Effect in Non-Small Cell Lung Cancer Cells.
Carcinoma, Renal Cell
Metabolic Modulation of Clear-cell Renal Cell Carcinoma with Dichloroacetate, an Inhibitor of Pyruvate Dehydrogenase Kinase.
Cardiomegaly
Apigenin ameliorates hypertension-induced cardiac hypertrophy and down-regulates cardiac hypoxia inducible factor-l? in rats.
Nuclear factor-kappaB activation leads to down-regulation of fatty acid oxidation during cardiac hypertrophy.
Preventive effects of L-glutamine on gestational fructose-induced cardiac hypertrophy: Involvement of pyruvate dehydrogenase kinase-4.
Reactivation of peroxisome proliferator-activated receptor alpha is associated with contractile dysfunction in hypertrophied rat heart.
The interplay between NF-kappaB and E2F1 coordinately regulates inflammation and metabolism in human cardiac cells.
Cardiomyopathies
A review of the underlying genetics and emerging therapies for canine cardiomyopathies.
Overexpression of pyruvate dehydrogenase kinase 4 in heart perturbs metabolism and exacerbates calcineurin-induced cardiomyopathy.
Cardiomyopathy, Dilated
A missense variant in the titin gene in Doberman pinscher dogs with familial dilated cardiomyopathy and sudden cardiac death.
Functional Consequences of PDK4 Deficiency in Doberman Pinscher Fibroblasts.
In vitro evaluation of mitochondrial dysfunction and treatment with adeno-associated virus vector in fibroblasts from Doberman Pinschers with dilated cardiomyopathy and a pyruvate dehydrogenase kinase 4 mutation.
Charcot-Marie-Tooth Disease
A new locus for X-linked dominant Charcot-Marie-Tooth disease (CMTX6) is caused by mutations in the pyruvate dehydrogenase kinase isoenzyme 3 (PDK3) gene.
Charcot-Marie-tooth disease causing mutation (p.R158H) in pyruvate dehydrogenase kinase 3 (PDK3) affects synaptic transmission, ATP production and causes neurodegeneration in a CMTX6 C. elegans model.
X-linked Charcot-Marie-Tooth disease type 6 (CMTX6) patients with a p.R158H mutation in the pyruvate dehydrogenase kinase isoenzyme 3 gene.
Cholangiocarcinoma
Serum pyruvate dehydrogenase kinase as a prognostic marker for cholangiocarcinoma.
Cholestasis
MITOCHONDRIAL BIOGENESIS FAILS IN SECONDARY BILIARY CIRRHOSIS IN RATS LEADING TO MITOCHONDRIAL DNA DEPLETION AND DELETIONS.
Colonic Neoplasms
Interactions between PPAR Gamma and the Canonical Wnt/Beta-Catenin Pathway in Type 2 Diabetes and Colon Cancer.
Overexpression of pyruvate dehydrogenase kinase 3 increases drug resistance and early recurrence in colon cancer.
Transforming Growth Factor ? Mediates Drug Resistance by Regulating the Expression of Pyruvate Dehydrogenase Kinase 4 in Colorectal Cancer.
Colorectal Neoplasms
Crosstalk among proteome, acetylome and succinylome in colon cancer HCT116 cell treated with sodium dichloroacetate.
Dichloroacetate induces apoptosis and cell-cycle arrest in colorectal cancer cells.
Hemistepsin A suppresses colorectal cancer growth through inhibiting pyruvate dehydrogenase kinase activity.
Pyruvate dehydrogenase kinase 4 exhibits a novel role in the activation of mutant KRAS, regulating cell growth in lung and colorectal tumour cells.
Pyruvate dehydrogenase kinase expression and metabolic changes following dichloroacetate exposure in anoxic human colorectal cancer cells.
The combined effect of dichloroacetate and 3-bromopyruvate on glucose metabolism in colorectal cancer cell line, HT-29; the mitochondrial pathway apoptosis.
Transforming Growth Factor ? Mediates Drug Resistance by Regulating the Expression of Pyruvate Dehydrogenase Kinase 4 in Colorectal Cancer.
Withdrawal: Transforming growth factor ? mediates drug resistance by regulating the expression of pyruvate dehydrogenase kinase 4 in colorectal cancer.
Coma
Changes in pyruvate dehydrogenase complex activity during and following severe insulin-induced hypoglycemia.
Coronary Occlusion
Dichloroacetate attenuates myocardial acidosis and metabolic changes induced by partial occlusion of the coronary artery in dogs.
Diabetes Mellitus
Mitochondrial regulators of fatty acid metabolism reflect metabolic dysfunction in type 2 diabetes mellitus.
[Genetic polymorphism of pyruvate dehydrogenase kinase 4 (PDK4), paraoxonase 2 (PON2), and fatty acid binding protein 2 (FABP2) in the NIDDM population of Senegal]
Diabetes Mellitus, Type 2
Additive effects of clofibric acid and pyruvate dehydrogenase kinase isoenzyme 4 (PDK4) deficiency on hepatic steatosis in mice fed a high saturated fat diet.
Association of pyruvate dehydrogenase kinase 4 gene polymorphisms with type 2 diabetes and metabolic syndrome.
AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2.
Mitochondrial regulators of fatty acid metabolism reflect metabolic dysfunction in type 2 diabetes mellitus.
Pyruvate dehydrogenase kinase isoenzyme 4 (PDHK4) deficiency attenuates the long-term negative effects of a high-saturated fat diet.
[Genetic polymorphism of pyruvate dehydrogenase kinase 4 (PDK4), paraoxonase 2 (PON2), and fatty acid binding protein 2 (FABP2) in the NIDDM population of Senegal]
Diabetic Neuropathies
Satellite glia as a critical component of diabetic neuropathy: Role of lipocalin-2 and pyruvate dehydrogenase kinase-2 axis in the dorsal root ganglion.
Dyslipidemias
Effects of neonatal dexamethasone administration on cardiac recovery ability under ischemia-reperfusion in 24 weeks old rats.
Encephalomyelitis
Metabolic programming and PDHK1 control CD4+ T cell subsets and inflammation.
Encephalomyelitis, Autoimmune, Experimental
Metabolic programming and PDHK1 control CD4+ T cell subsets and inflammation.
Endometriosis
Repurposing dichloroacetate for the treatment of women with endometriosis.
Esophageal Neoplasms
Associations of PGK1 promoter hypomethylation and PGK1-mediated PDHK1 phosphorylation with cancer stage and prognosis: a TCGA pan-cancer analysis.
Fatty Liver
Induction of PDK4 in the heart muscle of JVS mice, an animal model of systemic carnitine deficiency, does not appear to reduce glucose utilization by the heart.
Pyruvate dehydrogenase kinase 4 mRNA is increased in the hypertrophied ventricles of carnitine-deficient juvenile visceral steatosis (JVS) mice.
Glioblastoma
Carnosine influences transcription via epigenetic regulation as demonstrated by enhanced histone acetylation of the pyruvate dehydrogenase kinase 4 promoter in glioblastoma cells.
Combined targeting of PDK1 and EGFR triggers regression of glioblastoma by reversing the Warburg effect.
Identification of a novel non-ATP-competitive protein kinase inhibitor of PGK1 from marine nature products.
IDH1 Mutation Induces Reprogramming of Pyruvate Metabolism.
Metabolic modulation of glioblastoma with dichloroacetate.
Metabolic-targeted Combination Therapy With Dichloroacetate and Metformin Suppresses Glioblastoma Cell Line Growth In Vitro and In Vivo.
Mitochondria-Translocated PGK1 Functions as a Protein Kinase to Coordinate Glycolysis and the TCA Cycle in Tumorigenesis.
Glioma
Nodal regulates energy metabolism in glioma cells by inducing expression of hypoxia-inducible factor 1?.
Pyruvate dehydrogenase kinase as a potential therapeutic target for malignant gliomas.
Glucose Intolerance
Pyruvate dehydrogenase kinase isoenzyme 4 (PDHK4) deficiency attenuates the long-term negative effects of a high-saturated fat diet.
Graves Ophthalmopathy
PDK2-enhanced glycolysis promotes fibroblast proliferation in thyroid-associated ophthalmopathy.
Head and Neck Neoplasms
Hypoxic repression of pyruvate dehydrogenase activity is necessary for metabolic reprogramming and growth of model tumours.
Heart Diseases
Increased Expression of PDK4 Was Displayed in Gastric Cancer and Exhibited an Association With Glucose Metabolism.
Heart Failure
Increasing carbohydrate oxidation improves contractile reserves and prevents hypertrophy in porcine right heart failure.
Targeting mitochondrial oxidative metabolism as an approach to treat heart failure.
The interplay between NF-kappaB and E2F1 coordinately regulates inflammation and metabolism in human cardiac cells.
Hepatitis C
Pyruvate dehydrogenase kinase regulates hepatitis C virus replication.
Hyperglycemia
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Oral ethinylestradiol-levonorgestrel attenuates cardiac glycogen and triglyceride accumulation in high fructose female rats by suppressing pyruvate dehydrogenase kinase-4.
Pyruvate dehydrogenase kinase isoenzyme 4 (PDHK4) deficiency attenuates the long-term negative effects of a high-saturated fat diet.
Hypersensitivity
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Hypertension
Increased Pyruvate Dehydrogenase Kinase 4 Expression in Lung Pericytes Is Associated with Reduced Endothelial-Pericyte Interactions and Small Vessel Loss in Pulmonary Arterial Hypertension.
Inhibition of pyruvate dehydrogenase kinase improves pulmonary arterial hypertension in genetically susceptible patients.
Hypertension, Pulmonary
FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4 (PDK4) decreases glucose oxidation and impairs right ventricular function in pulmonary hypertension: therapeutic benefits of dichloroacetate.
Hyperthyroidism
Evaluation of the role of peroxisome-proliferator-activated receptor alpha in the regulation of cardiac pyruvate dehydrogenase kinase 4 protein expression in response to starvation, high-fat feeding and hyperthyroidism.
Expression and regulation of pyruvate dehydrogenase kinase isoforms in the developing rat heart and in adulthood: role of thyroid hormone status and lipid supply.
Increased hepatic pyruvate dehydrogenase kinase activity in fed hyperthyroid rats: studies in vivo and with cultured hepatocytes.
Interactive effects of insulin and triiodothyronine on pyruvate dehydrogenase kinase activity in cardiac myocytes.
Pyruvate inhibition of pyruvate dehydrogenase kinase. Effects of progressive starvation and hyperthyroidism in vivo, and of dibutyryl cyclic AMP and fatty acids in cultured cardiac myocytes.
Regulation of renal and hepatic pyruvate dehydrogenase complex on carbohydrate re-feeding after starvation. Possible mechanisms and a regulatory role for thyroid hormone.
Role of pyruvate dehydrogenase inhibition in the development of hypertrophy in the hyperthyroid rat heart: a combined magnetic resonance imaging and hyperpolarized magnetic resonance spectroscopy study.
Selective modification of the pyruvate dehydrogenase kinase isoform profile in skeletal muscle in hyperthyroidism: implications for the regulatory impact of glucose on fatty acid oxidation.
Hypertrophy, Right Ventricular
FOXO1-mediated upregulation of pyruvate dehydrogenase kinase-4 (PDK4) decreases glucose oxidation and impairs right ventricular function in pulmonary hypertension: therapeutic benefits of dichloroacetate.
The inhibition of pyruvate dehydrogenase kinase improves impaired cardiac function and electrical remodeling in two models of right ventricular hypertrophy: resuscitating the hibernating right ventricle.
Hypoglycemia
Cardiac failure in C5-deficient A/J mice after Candida albicans infection.
Naloxone, but not valsartan, preserves responses to hypoglycemia after antecedent hypoglycemia: Role of metabolic reprogramming in counterregulatory failure.
The Effects of Sodium Dichloroacetate on Mitochondrial Dysfunction and Neuronal Death Following Hypoglycemia-Induced Injury.
Immune System Diseases
MicroRNA -148 alleviates cardiac dysfunction, immune disorders and myocardial apoptosis in myocardial ischemia-reperfusion (MI/R) injury by targeting pyruvate dehydrogenase kinase (PDK4).
Infections
iTRAQ-based proteomic profile analysis of ISKNV-infected CPB cells with emphasizing on glucose metabolism, apoptosis and autophagy pathways.
Influenza, Human
Diisopropylamine dichloroacetate, a novel pyruvate dehydrogenase kinase 4 inhibitor, as a potential therapeutic agent for metabolic disorders and multiorgan failure in severe influenza.
Insulin Resistance
Altered cardiac fatty acid composition and utilization following dexamethasone-induced insulin resistance.
Capric Acid Up-Regulates UCP3 Expression without PDK4 Induction in Mouse C2C12 Myotubes.
Differential regulation of metabolic genes in skeletal muscle during starvation and refeeding in humans.
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Fasting induces ketoacidosis and hypothermia in PDHK2/PDHK4 double knockout mice.
Impaired expression of NADH dehydrogenase subunit 1 and PPARgamma coactivator-1 in skeletal muscle of ZDF rats: restoration by troglitazone.
Increased hepatic pyruvate dehydrogenase kinase activity in fed hyperthyroid rats: studies in vivo and with cultured hepatocytes.
Inhibition of pyruvate dehydrogenase kinase 2 protects against hepatic steatosis through modulation of TCA cycle anaplerosis and ketogenesis.
Metabolic diseases drug discovery world summit. July 28-29, 2003, San Diego, CA, USA.
Perpetual muscle PDH activation in PDH kinase knockout mice protects against high-fat feeding-induced muscle insulin resistance.
Preoperative carbohydrate supplementation attenuates post-surgery insulin resistance via reduced inflammatory inhibition of the insulin-mediated restraint on muscle pyruvate dehydrogenase kinase 4 expression.
Pyruvate dehydrogenase kinase 4 (PDK4) could be involved in a regulatory role in apoptosis and a link between apoptosis and insulin resistance.
The effect of insulin on the uptake and metabolic fate of glucose in isolated perfused hearts of dyslipemic rats.
The pyruvate dehydrogenase complex: nutrient control and the pathogenesis of insulin resistance.
[Effects of competitive substrates ans insulin on glucose uptake and utilization in isolated perfused hearts of dyslipemic rats]
Iron Overload
Effects of iron loading on muscle: genome-wide mRNA expression profiling in the mouse.
Ischemic Stroke
Sodium Dichloroacetate Stimulates Angiogenesis by Improving Endothelial Precursor Cell Function in an AKT/GSK-3?/Nrf2 Dependent Pathway in Vascular Dementia Rats.
Lung Neoplasms
Blocking Aerobic Glycolysis by Targeting Pyruvate Dehydrogenase Kinase in Combination with EGFR TKI and Ionizing Radiation Increases Therapeutic Effect in Non-Small Cell Lung Cancer Cells.
Discovery of Hordenine as a Potential Inhibitor of Pyruvate Dehydrogenase Kinase 3: Implication in Lung Cancer Therapy.
Liquid Chromatography-Tandem Mass Spectrometry Method Revealed that Lung Cancer Cells Exhibited Distinct Metabolite Profiles upon the Treatment with Different Pyruvate Dehydrogenase Kinase Inhibitors.
Pyruvate dehydrogenase and pyruvate dehydrogenase kinase expression in non small cell lung cancer and tumor-associated stroma.
Suppression of pyruvate dehydrogenase kinase-2 re-sensitizes paclitaxel-resistant human lung cancer cells to paclitaxel.
Water-extracted branch of Cinnamomum cassia promotes lung cancer cell apoptosis by inhibiting pyruvate dehydrogenase kinase activity.
Lymphoma
Novel molecular mechanisms of antitumor action of dichloroacetate against T cell lymphoma: Implication of altered glucose metabolism, pH homeostasis and cell survival regulation.
Lymphoma, B-Cell
Effect of Huaier on the proliferation and apoptosis of human gastric cancer cells through modulation of the PI3K/AKT signaling pathway.
Pyruvate dehydrogenase kinase 4-mediated metabolic reprogramming is involved in rituximab resistance in diffuse large B-cell lymphoma by affecting the expression of MS4A1/CD20.
The effects of the 5-HT2A receptor antagonist sarpogrelate hydrochloride on chronic hypoxic pulmonary hypertension in rats.
Lymphoma, Large B-Cell, Diffuse
Pyruvate dehydrogenase kinase 4-mediated metabolic reprogramming is involved in rituximab resistance in diffuse large B-cell lymphoma by affecting the expression of MS4A1/CD20.
Lymphoma, T-Cell
Novel molecular mechanisms of antitumor action of dichloroacetate against T cell lymphoma: Implication of altered glucose metabolism, pH homeostasis and cell survival regulation.
Melanoma
Bioenergetic modulation with dichloroacetate reduces the growth of melanoma cells and potentiates their response to BRAFV600E inhibition.
Overexpression of pyruvate dehydrogenase kinase supports dichloroacetate as a candidate for cutaneous melanoma therapy.
Metabolic Diseases
Correction to Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Metabolic Syndrome
Association of pyruvate dehydrogenase kinase 4 gene polymorphisms with type 2 diabetes and metabolic syndrome.
Muscle Weakness
Reduction of mitochondria and up regulation of pyruvate dehydrogenase kinase 4 of skeletal muscle in patients with chronic kidney disease.
Muscular Atrophy
A potential role for Akt/FOXO signalling in both protein loss and the impairment of muscle carbohydrate oxidation during sepsis in rodent skeletal muscle.
Interaction of contractile activity and training history on mRNA abundance in skeletal muscle from trained athletes.
Muscular Diseases
Pharmacological activation of the pyruvate dehydrogenase complex reduces statin-mediated upregulation of FOXO gene targets and protects against statin myopathy in rodents.
Myasthenia Gravis
Molecular profiling of thymoma with myasthenia gravis: Risk factors of developing myasthenia gravis in thymoma patients.
Myocardial Stunning
Brief increase in carbohydrate oxidation after reperfusion reverses myocardial stunning in conscious pigs.
Neoplasm Metastasis
Ascites-derived ALDH+CD44+ tumour cell subsets endow stemness, metastasis and metabolic switch via PDK4-mediated STAT3/AKT/NF-?B/IL-8 signalling in ovarian cancer.
Loss of the novel mitochondrial protein FAM210B promotes metastasis via PDK4-dependent metabolic reprogramming.
Novel molecular mechanisms of antitumor action of dichloroacetate against T cell lymphoma: Implication of altered glucose metabolism, pH homeostasis and cell survival regulation.
Pyruvate dehydrogenase kinase 1 and carbonic anhydrase IX targeting in hypoxic tumors.
Targeted reversal and phosphorescence lifetime imaging of cancer cell metabolism via a theranostic rhenium(I)-DCA conjugate.
Neoplasms
(1)H NMR metabolomics analysis of the effect of dichloroacetate and allopurinol on breast cancers.
?-Asarone Increases Chemosensitivity by Inhibiting Tumor Glycolysis in Gastric Cancer.
A Mechanism-Based Pharmacokinetic Enzyme Turnover Model for Dichloroacetic Acid Autoinhibition in Rats.
A mitochondria-K+ channel axis is suppressed in cancer and its normalization promotes apoptosis and inhibits cancer growth.
A potent tumoricidal co-drug 'Bet-CA'--an ester derivative of betulinic acid and dichloroacetate selectively and synergistically kills cancer cells.
Acquired Mitochondrial Abnormalities, Including Epigenetic Inhibition of Superoxide Dismutase 2, in Pulmonary Hypertension and Cancer: Therapeutic Implications.
Adding a combination of hydroxycitrate and lipoic acid (METABLOC™) to chemotherapy improves effectiveness against tumor development: experimental results and case report.
AG311, a small molecule inhibitor of complex I and hypoxia-induced HIF-1? stabilization.
Altered promoter methylation of PDK4, IL1 B, IL6, and TNF after Roux-en Y gastric bypass.
Anemone rivularis inhibits pyruvate dehydrogenase kinase activity and tumor growth.
Anti-breast Cancer Enhancement of a Polysaccharide From Spore of Ganoderma lucidum With Paclitaxel: Suppression on Tumor Metabolism With Gut Microbiota Reshaping.
Anti-cancer synergy of dichloroacetate and EGFR tyrosine kinase inhibitors in NSCLC cell lines.
Antitumor and chemosensitizing action of dichloroacetate implicates modulation of tumor microenvironment: A role of reorganized glucose metabolism, cell survival regulation and macrophage differentiation.
Are peroxisome proliferator-activated receptors involved in skeletal muscle wasting during experimental cancer cachexia? Role of beta2-adrenergic agonists.
Ascites-derived ALDH+CD44+ tumour cell subsets endow stemness, metastasis and metabolic switch via PDK4-mediated STAT3/AKT/NF-?B/IL-8 signalling in ovarian cancer.
Associations of PGK1 promoter hypomethylation and PGK1-mediated PDHK1 phosphorylation with cancer stage and prognosis: a TCGA pan-cancer analysis.
Bevacizumab treatment induces metabolic adaptation toward anaerobic metabolism in glioblastomas.
Cancer cell metabolism: implications for therapeutic targets.
Comparison of spheroids formed by rat glioma stem cells and neural stem cells reveals differences in glucose metabolism and promising therapeutic applications.
Crosstalk among proteome, acetylome and succinylome in colon cancer HCT116 cell treated with sodium dichloroacetate.
Dichloroacetate affects proliferation but not apoptosis in canine mammary cell lines.
Dichloroacetate induces tumor-specific radiosensitivity in vitro but attenuates radiation-induced tumor growth delay in vivo.
Dichloroacetate potentiates tamoxifen-induced cell death in breast cancer cells via downregulation of the epidermal growth factor receptor.
Dichloroacetate should be considered with platinum-based chemotherapy in hypoxic tumors rather than as a single agent in advanced non-small cell lung cancer.
Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90.
Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases.
Discovery of potent pyruvate dehydrogenase kinase inhibitors and evaluation of their anti-lung cancer activity under hypoxia.
Effect of pH on the structure and function of pyruvate dehydrogenase kinase 3: Combined spectroscopic and MD simulation studies.
Effects of recombinant monokines on hepatic pyruvate dehydrogenase, pyruvate dehydrogenase kinase, lipogenesis de novo and plasma triacylglycerols. Abolition by prior fasting.
Effects of three modifiers of glycolysis on ATP, lactate, hypoxia, and growth in human tumor cell lines in vivo.
Expression and clinical significance of PDK family in breast cancer based on data mining.
Flavonoids Targeting HIF-1: Implications on Cancer Metabolism.
Flicking the Warburg switch-tyrosine phosphorylation of pyruvate dehydrogenase kinase regulates mitochondrial activity in cancer cells.
Hemistepsin A suppresses colorectal cancer growth through inhibiting pyruvate dehydrogenase kinase activity.
Huzhangoside A Suppresses Tumor Growth through Inhibition of Pyruvate Dehydrogenase Kinase Activity.
Hyaluronan matrix inhibition enhances metabolic anticancer therapy by dichloroacetate in vitro and in vivo.
Hypoxic repression of pyruvate dehydrogenase activity is necessary for metabolic reprogramming and growth of model tumours.
Identification of high-affinity inhibitors of pyruvate dehydrogenase kinase-3: towards therapeutic management of cancer.
In vitro cytotoxicity of combinations of dichloroacetate with anticancer platinum compounds.
Increasing Superoxide Production and the Labile Iron Pool in Tumor Cells may Sensitize Them to Extracellular Ascorbate.
Inhibition of Pyruvate Dehydrogenase Kinase as a Therapeutic Strategy against Cancer.
Inhibition of Pyruvate Dehydrogenase Kinase Enhances the Antitumor Efficacy of Oncolytic Reovirus.
Investigation of inhibitory potential of quercetin to the pyruvate dehydrogenase kinase 3: Towards implications in anticancer therapy.
Isolation of expressed sequence tags of skeletal muscle of neonatal healthy and splay leg piglets and mapping by somatic cell hybrid analysis.
JX06 Selectively Inhibits Pyruvate Dehydrogenase Kinase PDK1 by a Covalent Cysteine Modification.
LINC00662 modulates cervical cancer cell proliferation, invasion, and apoptosis via sponging miR-103a-3p and upregulating PDK4.
Loss of PDK4 expression promotes proliferation, tumorigenicity, motility and invasion of hepatocellular carcinoma cells.
Lung Cancer: A Comparative Study of Metabolism Related Protein Expression in Cancer Cells and Tumor Associated Stroma.
Mathematical modeling links Wnt signaling to emergent patterns of metabolism in colon cancer.
Metabolic and transcriptional profiling reveals pyruvate dehydrogenase kinase 4 as a mediator of epithelial-mesenchymal transition and drug resistance in tumor cells.
Metabolic cooperation between co-cultured lung cancer cells and lung fibroblasts.
Metabolic enzyme PDK3 forms a positive feedback loop with transcription factor HSF1 to drive chemoresistance.
Metabolic Flexibility in Cancer: Targeting the Pyruvate Dehydrogenase Kinase:Pyruvate Dehydrogenase Axis.
Metabolic modulation of cancer: a new frontier with great translational potential.
Metabolic targeting as an anticancer strategy: dawn of a new era?
Microenvironmental control of glucose metabolism in tumors by regulation of pyruvate dehydrogenase.
microRNA-129-5p, a c-Myc negative target, affects hepatocellular carcinoma progression by blocking the Warburg effect.
MicroRNA-214 suppresses cell proliferation and migration and cell metabolism by targeting PDK2 and PHF6 in hepatocellular carcinoma.
MiR-422a regulates cellular metabolism and malignancy by targeting pyruvate dehydrogenase kinase 2 in gastric cancer.
Mitaplatin, a potent fusion of cisplatin and the orphan drug dichloroacetate.
Mitochondrial activation by inhibition of PDKII suppresses HIF1a signaling and angiogenesis in cancer.
Mitochondrial dysfunction in gliomas.
Mitochondrial metabolism, redox signaling, and fusion: a mitochondria-ROS-HIF-1alpha-Kv1.5 O2-sensing pathway at the intersection of pulmonary hypertension and cancer.
Multi-modality imaging to assess metabolic response to dichloroacetate treatment in tumor models.
Natural Product Albiziabioside A Conjugated with Pyruvate Dehydrogenase Kinase Inhibitor Dichloroacetate to Induce Apoptosis-Ferroptosis M2-TAMs Polarization for Combined Cancer Therapy.
Novel molecular mechanisms of antitumor action of dichloroacetate against T cell lymphoma: Implication of altered glucose metabolism, pH homeostasis and cell survival regulation.
Overexpression of PDK2 and PDK3 reflects poor prognosis in acute myeloid leukemia.
Overexpression of PDK4 is associated with cell proliferation, drug resistance and poor prognosis in ovarian cancer.
Overexpression of pyruvate dehydrogenase kinase supports dichloroacetate as a candidate for cutaneous melanoma therapy.
PDK4 drives metabolic alterations and muscle atrophy in cancer cachexia.
Pro-haloacetate Nanoparticles for Efficient Cancer Therapy via Pyruvate Dehydrogenase Kinase Modulation.
Protein-bound NAD(P)H Lifetime is Sensitive to Multiple Fates of Glucose Carbon.
Pyruvate dehydrogenase kinase 1 and carbonic anhydrase IX targeting in hypoxic tumors.
Pyruvate Dehydrogenase Kinase 4 Deficiency Results in Expedited Cellular Proliferation through E2F1-Mediated Increase of Cyclins.
Pyruvate dehydrogenase kinase 4 exhibits a novel role in the activation of mutant KRAS, regulating cell growth in lung and colorectal tumour cells.
Pyruvate dehydrogenase kinase as a novel therapeutic target in oncology.
Pyruvate dehydrogenase kinase expression and metabolic changes following dichloroacetate exposure in anoxic human colorectal cancer cells.
Pyruvate dehydrogenase kinase regulatory mechanisms and inhibition in treating diabetes, heart ischemia, and cancer.
Reversal of the glycolytic phenotype by dichloroacetate inhibits metastatic breast cancer cell growth in vitro and in vivo.
Salinomycin and dichloroacetate synergistically inhibit Lewis lung carcinoma cell proliferation, tumor growth and metastasis.
Sensitization of metformin-cytotoxicity by dichloroacetate via reprogramming glucose metabolism in cancer cells.
Serum pyruvate dehydrogenase kinase as a prognostic marker for cholangiocarcinoma.
Sodium dichloroacetate attenuates the growth of B16-F10 melanoma in vitro and in vivo: an opportunity for drug repurposing.
Suppression of Pyruvate Dehydrogenase Kinase by Dichloroacetate in Cancer and Skeletal Muscle Cells Is Isoform Specific and Partially Independent of HIF-1?.
Suppression of pyruvate dehydrogenase kinase-2 re-sensitizes paclitaxel-resistant human lung cancer cells to paclitaxel.
Synergistic antitumor effect of dichloroacetate in combination with 5-Fluorouracil in colorectal cancer.
Synthetic Essentiality of Metabolic Regulator PDHK1 in PTEN-Deficient Cells and Cancers.
Targeted reversal and phosphorescence lifetime imaging of cancer cell metabolism via a theranostic rhenium(I)-DCA conjugate.
Targeting cellular metabolism to improve cancer therapeutics.
Targeting pyruvate dehydrogenase kinase signaling in the development of effective cancer therapy.
The miR-15b-5p/PDK4 axis regulates osteosarcoma proliferation through modulation of the Warburg effect.
The transcriptional co-repressor myeloid translocation gene 16 inhibits glycolysis and stimulates mitochondrial respiration.
Therapeutic Targeting of the Pyruvate Dehydrogenase Complex/Pyruvate Dehydrogenase Kinase (PDC/PDK) Axis in Cancer.
Thiamine mimetics sulbutiamine and benfotiamine as a nutraceutical approach to anticancer therapy.
Treatment of Pancreatic Cancer Patient-Derived Xenograft Panel with Metabolic Inhibitors Reveals Efficacy of Phenformin.
Two dichloric compounds inhibit in vivo U87 xenograft tumor growth.
Tyr-94 phosphorylation inhibits pyruvate dehydrogenase phosphatase 1 and promotes tumor growth.
Tyrosine phosphorylation of mitochondrial pyruvate dehydrogenase kinase 1 is important for cancer metabolism.
Unexpected Discovery of Dichloroacetate Derived Adenosine Triphosphate Competitors Targeting Pyruvate Dehydrogenase Kinase To Inhibit Cancer Proliferation.
VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells.
Water-extracted branch of Cinnamomum cassia promotes lung cancer cell apoptosis by inhibiting pyruvate dehydrogenase kinase activity.
Newcastle Disease
Targeting aerobic glycolysis by dichloroacetate improves Newcastle disease virus-mediated viro-immunotherapy in hepatocellular carcinoma.
Non-alcoholic Fatty Liver Disease
Pyruvate dehydrogenase kinase 4 mediates lipogenesis and contributes to the pathogenesis of nonalcoholic steatohepatitis.
Obesity
A novel inhibitor of pyruvate dehydrogenase kinase stimulates myocardial carbohydrate oxidation in diet-induced obesity.
Additive effects of clofibric acid and pyruvate dehydrogenase kinase isoenzyme 4 (PDK4) deficiency on hepatic steatosis in mice fed a high saturated fat diet.
Adipocyte pyruvate dehydrogenase kinase 4 expression is associated with augmented PPAR? upregulation in early-life programming of later obesity.
Inhibition of pyruvate dehydrogenase kinase-4 by l-glutamine protects pregnant rats against fructose-induced obesity and hepatic lipid accumulation.
Pyruvate dehydrogenase kinase isoenzyme 4 (PDHK4) deficiency attenuates the long-term negative effects of a high-saturated fat diet.
The role of pyruvate dehydrogenase kinase in diabetes and obesity.
Osteosarcoma
Fructose-coated Angstrom silver inhibits osteosarcoma growth and metastasis via promoting ROS-dependent apoptosis through the alteration of glucose metabolism by inhibiting PDK.
Ovarian Neoplasms
A comparative analysis of inhibitors of the glycolysis pathway in breast and ovarian cancer cell line models.
Pancreatic Neoplasms
Antitumor activity of potent pyruvate dehydrogenase kinase 4 inhibitors from plants in pancreatic cancer.
Inhibition of pyruvate dehydrogenase kinase influence microbiota and metabolomic profile in pancreatic cancer xenograft mice.
Metabolic checkpoint of ferroptosis resistance.
Peripheral Nervous System Diseases
Metabolic modulation of glioblastoma with dichloroacetate.
Pulmonary Arterial Hypertension
Increased Pyruvate Dehydrogenase Kinase 4 Expression in Lung Pericytes Is Associated with Reduced Endothelial-Pericyte Interactions and Small Vessel Loss in Pulmonary Arterial Hypertension.
Inhibition of pyruvate dehydrogenase kinase improves pulmonary arterial hypertension in genetically susceptible patients.
pyruvate decarboxylase deficiency
Increased superoxide accumulation in pyruvate dehydrogenase complex deficient fibroblasts.
pyruvate dehydrogenase (acetyl-transferring) deficiency
Reduction of mitochondria and up regulation of pyruvate dehydrogenase kinase 4 of skeletal muscle in patients with chronic kidney disease.
Pyruvate Dehydrogenase Complex Deficiency Disease
Reduction of mitochondria and up regulation of pyruvate dehydrogenase kinase 4 of skeletal muscle in patients with chronic kidney disease.
Renal Insufficiency, Chronic
Reduction of mitochondria and up regulation of pyruvate dehydrogenase kinase 4 of skeletal muscle in patients with chronic kidney disease.
Rhabdomyosarcoma
Increased fat oxidation and regulation of metabolic genes with ultraendurance exercise.
Seizures
Long-term expression of metabolism-associated genes in the rat hippocampus following recurrent neonatal seizures and its regulation by melatonin.
Sepsis
Increased pyruvate dehydrogenase kinase activity in response to sepsis.
LncRNA CASC2 Alleviates Sepsis-induced Acute Lung Injury by Regulating the miR-152-3p/PDK4 Axis.
PDK4 drives metabolic alterations and muscle atrophy in cancer cachexia.
Sepsis alters pyruvate dehydrogenase kinase activity in skeletal muscle.
TNF binding protein prevents hyperlactatemia and inactivation of PDH complex in skeletal muscle during sepsis.
Shock, Septic
Lipopolysaccharide (LPS)-induced septic shock causes profound changes in myocardial energy metabolites in pigs.
Small Cell Lung Carcinoma
Pyruvate dehydrogenase and pyruvate dehydrogenase kinase expression in non small cell lung cancer and tumor-associated stroma.
Starvation
A new family of protein kinases--the mitochondrial protein kinases.
Adaptive increase in pyruvate dehydrogenase kinase 4 during starvation is mediated by peroxisome proliferator-activated receptor alpha.
Control of muscle pyruvate oxidation during late pregnancy.
Cyclic AMP and free fatty acids in the longer-term regulation of pyruvate dehydrogenase kinase in rat soleus muscle.
Differential regulation of metabolic genes in skeletal muscle during starvation and refeeding in humans.
Effects of aging on the activities of pyruvate dehydrogenase complex and its kinase in rat heart.
Enhanced activity of pyruvate dehydrogenase kinase in rat heart mitochondria in alloxan-diabetes or starvation.
Evaluation of the role of peroxisome-proliferator-activated receptor alpha in the regulation of cardiac pyruvate dehydrogenase kinase 4 protein expression in response to starvation, high-fat feeding and hyperthyroidism.
Fibre-type specific modification of the activity and regulation of skeletal muscle pyruvate dehydrogenase kinase (PDK) by prolonged starvation and refeeding is associated with targeted regulation of PDK isoenzyme 4 expression.
Glucose fatty acid interactions and the regulation of glucose disposal.
Inactivation of pyruvate dehydrogenase complex in heart muscle mitochondria of gold-thioglucose-induced obese mice is not due to a stable increase in activity of pyruvate dehydrogenase kinase.
Insulin reverses effects of starvation on the activity of pyruvate dehydrogenase kinase in cultured hepatocytes.
Insulin suppresses PDK-4 expression in skeletal muscle independently of plasma FFA.
Kinase activator protein mediates longer-term effects of starvation on activity of pyruvate dehydrogenase kinase in rat liver mitochondria.
Longer-term regulation of pyruvate dehydrogenase kinase in cultured rat hepatocytes.
Mechanism responsible for inactivation of skeletal muscle pyruvate dehydrogenase complex in starvation and diabetes.
Molecular mechanisms regulating myocardial glucose oxidation.
Nutrient deprivation induces the Warburg effect through ROS/AMPK-dependent activation of pyruvate dehydrogenase kinase.
Nutritional regulation of the protein kinases responsible for the phosphorylation of the alpha-ketoacid dehydrogenase complexes.
PDK4 drives metabolic alterations and muscle atrophy in cancer cachexia.
Persistent effects of starvation on pyruvate dehydrogenase kinase and phosphatase of lactating rat mammary gland [proceedings]
Protein kinase B-alpha inhibits human pyruvate dehydrogenase kinase-4 gene induction by dexamethasone through inactivation of FOXO transcription factors.
Pyruvate dehydrogenase kinase/activator in rat heart mitochondria, Assay, effect of starvation, and effect of protein-synthesis inhibitors of starvation.
Pyruvate inhibition of pyruvate dehydrogenase kinase. Effects of progressive starvation and hyperthyroidism in vivo, and of dibutyryl cyclic AMP and fatty acids in cultured cardiac myocytes.
Regulation of hepatic pyruvate dehydrogenase kinase by insulin and dietary manipulation in vivo. Studies with the euglycaemic-hyperinsulinaemic clamp.
Retinoic acids and trichostatin A (TSA), a histone deacetylase inhibitor, induce human pyruvate dehydrogenase kinase 4 (PDK4) gene expression.
Reversible phosphorylation of pyruvate dehydrogenase in rat skeletal-muscle mitochondria. Effects of starvation and diabetes.
Role of peroxisome proliferator-activated receptor-alpha in the mechanism underlying changes in renal pyruvate dehydrogenase kinase isoform 4 protein expression in starvation and after refeeding.
Role of protein synthesis and of fatty acid metabolism in the longer-term regulation of pyruvate dehydrogenase kinase.
Role of pyruvate dehydrogenase kinase isoenzyme 4 (PDHK4) in glucose homoeostasis during starvation.
Selective modification of pyruvate dehydrogenase kinase isoform expression in rat pancreatic islets elicited by starvation and activation of peroxisome proliferator-activated receptor-alpha: implications for glucose-stimulated insulin secretion.
Starvation and diabetes increase the amount of pyruvate dehydrogenase kinase isoenzyme 4 in rat heart.
Starvation increases the amount of pyruvate dehydrogenase kinase in several mammalian tissues.
Starvation of lactating rats leads to alterations in the behaviour of pyruvate dehydrogenase kinase which persist in the semi-purified pyruvate dehydrogenase complex of the mammary gland but are partly reversible in vitro.
Studies of the long-term regulation of hepatic pyruvate dehydrogenase kinase.
Substrate interactions in the short- and long-term regulation of renal glucose oxidation.
The roles of intrinsic kinase and of kinase/activator protein in the enhanced phosphorylation of pyruvate dehydrogenase complex in starvation.
Stomach Neoplasms
Associations of PGK1 promoter hypomethylation and PGK1-mediated PDHK1 phosphorylation with cancer stage and prognosis: a TCGA pan-cancer analysis.
MiR-422a regulates cellular metabolism and malignancy by targeting pyruvate dehydrogenase kinase 2 in gastric cancer.
MiR-5683 suppresses glycolysis and proliferation through targeting pyruvate dehydrogenase kinase 4 in gastric cancer.
Thymoma
Molecular profiling of thymoma with myasthenia gravis: Risk factors of developing myasthenia gravis in thymoma patients.
Urinary Bladder Neoplasms
Cryptotanshinone, a novel PDK 4 inhibitor, suppresses bladder cancer cell invasiveness via the mTOR/??catenin/N?cadherin axis.
The Role of Pyruvate Dehydrogenase Kinase-4 (PDK4) in Bladder Cancer and Chemoresistance.
Vascular Calcification
Corrigendum: Pyruvate Dehydrogenase Kinase 4 Promotes Vascular Calcification via SMAD1/5/8 Phosphorylation.
Mechanisms of Vascular Calcification: The Pivotal Role of Pyruvate Dehydrogenase Kinase 4.
Pyruvate Dehydrogenase Kinase 4 Promotes Vascular Calcification via SMAD1/5/8 Phosphorylation.
[pyruvate dehydrogenase (acetyl-transferring)] kinase deficiency
Fasting induces ketoacidosis and hypothermia in PDHK2/PDHK4 double knockout mice.
Pyruvate dehydrogenase kinase 4 deficiency attenuates cisplatin-induced acute kidney injury.
Pyruvate Dehydrogenase Kinase 4 Deficiency Results in Expedited Cellular Proliferation through E2F1-Mediated Increase of Cyclins.
Pyruvate dehydrogenase kinase isoenzyme 4 (PDHK4) deficiency attenuates the long-term negative effects of a high-saturated fat diet.
Pyruvate dehydrogenase kinase-4 deficiency lowers blood glucose and improves glucose tolerance in diet-induced obese mice.