Inhibition of lactate dehydrogenase activity as an approach to cancer therapy

The isoenzyme pattern of LDH does not play a physiological role; except perhaps during fast transitions in energy metabolism

(2016) Bjørn Quistorff et al.   Aging-US

Galloflavin suppresses lactate dehydrogenase activity and causes MYC downregulation in Burkitt lymphoma cells through NAD/NADH-dependent inhibition of sirtuin-1

(2013) Marina Vettraino et al.   ANTI-CANCER DRUGS

Identification of substituted 2-thio-6-oxo-1,6-dihydropyrimidines as inhibitors of human lactate dehydrogenase

(2013) Peter S. Dragovich et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Attenuation of LDHA expression in cancer cells leads to redox-dependent alterations in cytoskeletal structure and cell migration

(2013) Robert Arseneault et al.   CANCER LETTERS

Acidity Generated by the Tumor Microenvironment Drives Local Invasion

(2013) V. Estrella et al.   CANCER RESEARCH

Fragment Growing and Linking Lead to Novel Nanomolar Lactate Dehydrogenase Inhibitors

(2013) Anna Kohlmann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffolds

(2013) Carlotta Granchi et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Lactate Dehydrogenase-B Is Silenced by Promoter Methylation in a High Frequency of Human Breast Cancers

(2013) Nicola J. Brown et al.   PLoS One

Lactate dehydrogenase A is overexpressed in pancreatic cancer and promotes the growth of pancreatic cancer cells

(2013) Yefei Rong et al.   TUMOR BIOLOGY

Galloflavin prevents the binding of lactate dehydrogenase A to single stranded DNA and inhibits RNA synthesis in cultured cells

(2012) Luigi Fiume et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Integration of the metabolic/redox state, histone gene switching, DNA replication and S-phase progression by moonlighting metabolic enzymes

(2012) Hongpeng He et al.   BIOSCIENCE REPORTS

Inhibition of LDH-A by lentivirus-mediated small interfering RNA suppresses intestinal-type gastric cancer tumorigenicity through the downregulation of Oct4

(2012) Yongjie Zhang et al.   CANCER LETTERS

An Integrated Genomic Screen Identifies LDHB as an Essential Gene for Triple-Negative Breast Cancer

(2012) M. L. McCleland et al.   CANCER RESEARCH

Lactate Dehydrogenase B Is Required for the Growth of KRAS-Dependent Lung Adenocarcinomas

(2012) M. L. McCleland et al.   CLINICAL CANCER RESEARCH

Galloflavin, a new lactate dehydrogenase inhibitor, induces the death of human breast cancer cells with different glycolytic attitude by affecting distinct signaling pathways

(2012) F. Farabegoli et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Design and Synthesis of Novel Lactate Dehydrogenase A Inhibitors by Fragment-Based Lead Generation

(2012) Richard A. Ward et al.   JOURNAL OF MEDICINAL CHEMISTRY

A validated HPLC assay for the determination of R-(−)-gossypol in human plasma and its application in clinical pharmacokinetic studies

(2012) Hongxia Lin et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

LDHA is necessary for the tumorigenicity of esophageal squamous cell carcinoma

(2012) Feng Yao et al.   TUMOR BIOLOGY

Novel Role of NOX in Supporting Aerobic Glycolysis in Cancer Cells with Mitochondrial Dysfunction and as a Potential Target for Cancer Therapy

(2012) Weiqin Lu et al.   PLOS BIOLOGY

Randomized phase II trial of docetaxel plus prednisone in combination with placebo or AT-101, an oral small molecule Bcl-2 family antagonist, as first-line therapy for metastatic castration-resistant prostate cancer

(2011) G. Sonpavde et al.   ANNALS OF ONCOLOGY

LDH-A silencing suppresses breast cancer tumorigenicity through induction of oxidative stress mediated mitochondrial pathway apoptosis

(2011) Zhi-Yu Wang et al.   BREAST CANCER RESEARCH AND TREATMENT

Overcoming Trastuzumab Resistance in Breast Cancer by Targeting Dysregulated Glucose Metabolism

(2011) Y. Zhao et al.   CANCER RESEARCH

Lactate Dehydrogenase B Is Critical for Hyperactive mTOR-Mediated Tumorigenesis

(2011) X. Zha et al.   CANCER RESEARCH

The reverse Warburg effect: Aerobic glycolysis in cancer associated fibroblasts and the tumor stroma

(2011) Stephanos Pavlides et al.   CELL CYCLE

Galloflavin (CAS 568-80-9): A Novel Inhibitor of Lactate Dehydrogenase

(2011) Marcella Manerba et al.   ChemMedChem

Decreased lactate dehydrogenase B expression enhances claudin 1-mediated hepatoma cell invasiveness via mitochondrial defects

(2011) June-Hyung Kim et al.   EXPERIMENTAL CELL RESEARCH

Discovery ofN-Hydroxyindole-Based Inhibitors of Human Lactate Dehydrogenase Isoform A (LDH-A) as Starvation Agents against Cancer Cells

(2011) Carlotta Granchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antimalarial Activity of Potential Inhibitors of Plasmodium falciparum Lactate Dehydrogenase Enzyme Selected by Docking Studies

(2011) Julia Penna-Coutinho et al.   PLoS One

LDH-A influences hypoxia-inducible factor 1α (HIF1 α) and is critical for growth of HT29 colon carcinoma cells in vivo

(2011) Stefan Langhammer et al.   Targeted Oncology

Differences and similarities in binding of pyruvate and l-lactate in the active site of M4 and H4 isoforms of human lactate dehydrogenase

(2010) Katarzyna Świderek et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Targeting glycolysis: a fragment based approach towards bifunctional inhibitors of hLDH-5

(2010) Adam D. Moorhouse et al.   CHEMICAL COMMUNICATIONS

Inhibitors of Lactate Dehydrogenase Isoforms and their Therapeutic Potentials

(2010) C. Granchi et al.   CURRENT MEDICINAL CHEMISTRY

Warburg effect in chemosensitivity: Targeting lactate dehydrogenase-A re-sensitizes Taxol-resistant cancer cells to Taxol

(2010) Ming Zhou et al.   Molecular Cancer

The engine driving the ship: metabolic steering of cell proliferation and death

(2010) Marisa R. Buchakjian et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression

(2010) A. Le et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Evidence for an Alternative Glycolytic Pathway in Rapidly Proliferating Cells

(2010) M. G. Vander Heiden et al.   SCIENCE

The Control of the Metabolic Switch in Cancers by Oncogenes and Tumor Suppressor Genes

(2010) A. J. Levine et al.   SCIENCE

MYC-Induced Cancer Cell Energy Metabolism and Therapeutic Opportunities

(2009) C. V. Dang et al.   CLINICAL CANCER RESEARCH

Computational analyses of mammalian lactate dehydrogenases: Human, mouse, opossum and platypus LDHs

(2009) Roger S. Holmes et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

Cell-cell and intracellular lactate shuttles

(2009) George A. Brooks   JOURNAL OF PHYSIOLOGY-LONDON

D- and L-lactate dehydrogenases during invertebrate evolution

(2008) Melania E Cristescu et al.   BMC EVOLUTIONARY BIOLOGY

The Biology of Cancer: Metabolic Reprogramming Fuels Cell Growth and Proliferation

(2008) Ralph J. DeBerardinis et al.   Cell Metabolism

Mitochondria andl-lactate metabolism

(2008) Salvatore Passarella et al.   FEBS LETTERS

Histone 2B (H2B) Expression Is Confined to a Proper NAD+/NADH Redox Status

(2008) Ru-Ping Dai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Causes and Consequences of Increased Glucose Metabolism of Cancers

(2008) R. J. Gillies et al.   JOURNAL OF NUCLEAR MEDICINE

Pyruvate kinase M2 is a phosphotyrosine-binding protein

(2008) Heather R. Christofk et al.   NATURE

Mitochondrial Lactate Dehydrogenase Is Involved in Oxidative-Energy Metabolism in Human Astrocytoma Cells (CCF-STTG1)

(2008) Joseph Lemire et al.   PLoS One