Targeting lactate metabolism for cancer therapeutics

Glutamine supports pancreatic cancer growth through a KRAS-regulated metabolic pathway

(2013) Jaekyoung Son et al.   NATURE

Metabolic Reprogramming: A Cancer Hallmark Even Warburg Did Not Anticipate

(2012) Patrick S. Ward et al.   CANCER CELL

Lactate-Induced IL-8 Pathway in Endothelial Cells--Letter

(2012) C. Pinheiro et al.   CANCER RESEARCH

Reciprocal Metabolic Reprogramming through Lactate Shuttle Coordinately Influences Tumor-Stroma Interplay

(2012) T. Fiaschi et al.   CANCER RESEARCH

Mitochondrial metabolism in cancer metastasis

(2012) Federica Sotgia et al.   CELL CYCLE

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

Co-expression of monocarboxylate transporter 1 (MCT1) and its chaperone (CD147) is associated with low survival in patients with gastrointestinal stromal tumors (GISTs)

(2012) Antônio Talvane Torres de Oliveira et al.   JOURNAL OF BIOENERGETICS AND BIOMEMBRANES

Genome-wide RNA interference analysis of renal carcinoma survival regulators identifies MCT4 as a Warburg effect metabolic target

(2012) Marco Gerlinger et al.   JOURNAL OF PATHOLOGY

Monocarboxylate transporters (MCTs) in gliomas: expression and exploitation as therapeutic targets

(2012) Vera Miranda-Gonçalves et al.   NEURO-ONCOLOGY

Targeting the Lactate Transporter MCT1 in Endothelial Cells Inhibits Lactate-Induced HIF-1 Activation and Tumor Angiogenesis

(2012) Pierre Sonveaux et al.   PLoS One

Lactate Activates HIF-1 in Oxidative but Not in Warburg-Phenotype Human Tumor Cells

(2012) Christophe J. De Saedeleer et al.   PLoS One

Mouse Genetics Suggests Cell-Context Dependency for Myc-Regulated Metabolic Enzymes during Tumorigenesis

(2012) Lisa M. Nilsson et al.   PLoS Genetics

Monocarboxylate transporter 4 (MCT4) and CD147 overexpression is associated with poor prognosis in prostate cancer

(2011) Nelma Pértega-Gomes et al.   BMC CANCER

Regulation of Monocarboxylate Transporter MCT1 Expression by p53 Mediates Inward and Outward Lactate Fluxes in Tumors

(2011) R. Boidot et al.   CANCER RESEARCH

Lactate Influx through the Endothelial Cell Monocarboxylate Transporter MCT1 Supports an NF- B/IL-8 Pathway that Drives Tumor Angiogenesis

(2011) F. Vegran et al.   CANCER RESEARCH

Monocarboxylate transporters 1 and 4 are involved in the invasion activity of human lung cancer cells

(2011) Hiroto Izumi et al.   CANCER SCIENCE

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

(2011) Stephanos Pavlides et al.   CELL CYCLE

Evidence for a stromal-epithelial “lactate shuttle” in human tumors

(2011) Diana Whitaker-Menezes et al.   CELL CYCLE

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

(2011) Marcella Manerba et al.   ChemMedChem

Tumor lactic acidosis suppresses CTL function by inhibition of p38 and JNK/c-Jun activation

(2011) Anna N. Mendler et al.   INTERNATIONAL JOURNAL OF CANCER

The monocarboxylate transporter family-Structure and functional characterization

(2011) Andrew P. Halestrap   IUBMB LIFE

The monocarboxylate transporter family-Role and regulation

(2011) Andrew P. Halestrap et al.   IUBMB LIFE

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

A Phase II Study of AT-101 (Gossypol) in Chemotherapy-Sensitive Recurrent Extensive-Stage Small Cell Lung Cancer

(2011) Maria Q. Baggstrom et al.   Journal of Thoracic Oncology

miR-29a and miR-29b Contribute to Pancreatic  -Cell-Specific Silencing of Monocarboxylate Transporter 1 (Mct1)

(2011) T. J. Pullen et al.   MOLECULAR AND CELLULAR BIOLOGY

CD147 subunit of lactate/H+ symporters MCT1 and hypoxia-inducible MCT4 is critical for energetics and growth of glycolytic tumors

(2011) R. Le Floch et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of tumor lactate oxidation: Consequences for the tumor microenvironment

(2011) Morten Busk et al.   RADIOTHERAPY AND ONCOLOGY

The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein

(2010) Matthew J. Ovens et al.   BIOCHEMICAL JOURNAL

Understanding the "lethal" drivers of tumor-stroma co-evolution

(2010) Michael P. Lisanti et al.   CANCER BIOLOGY & THERAPY

The reverse Warburg Effect: Glycolysis inhibitors prevent the tumor promoting effects of caveolin-1 deficient cancer associated fibroblasts

(2010) Gloria Bonuccelli et al.   CELL CYCLE

Oxidative stress in cancer associated fibroblasts drives tumor-stroma co-evolution

(2010) Ubaldo E. Martinez-Outschoorn et al.   CELL CYCLE

Derepression of Polycomb targets during pancreatic organogenesis allows insulin-producing beta-cells to adopt a neural gene activity program

(2010) J. van Arensbergen et al.   GENOME RESEARCH

Monocarboxylate transporter 1 is up-regulated in basal-like breast carcinoma

(2010) Céline Pinheiro et al.   HISTOPATHOLOGY

IL-23-dependent and -independent enhancement pathways of IL-17A production by lactic acid

(2010) Masahiko Yabu et al.   INTERNATIONAL IMMUNOLOGY

Phase I/II Study of AT-101 with Topotecan in Relapsed and Refractory Small Cell Lung Cancer

(2010) Rebecca Suk Heist et al.   Journal of Thoracic Oncology

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

AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7–10

(2009) Matthew J. Ovens et al.   BIOCHEMICAL JOURNAL

An Open-Label, Multicenter, Phase I/II Study of Single-Agent AT-101 in Men with Castrate-Resistant Prostate Cancer

(2009) G. Liu et al.   CLINICAL CANCER RESEARCH

CD147 silencing inhibits lactate transport and reduces malignant potential of pancreatic cancer cells in in vivo and in vitro models

(2009) W Schneiderhan et al.   GUT

Lactic Acid and Acidification Inhibit TNF Secretion and Glycolysis of Human Monocytes

(2009) K. Dietl et al.   JOURNAL OF IMMUNOLOGY

LDH-A inhibition, a therapeutic strategy for treatment of hereditary leiomyomatosis and renal cell cancer

(2009) H. Xie et al.   MOLECULAR CANCER THERAPEUTICS

c-Myc suppression of miR-23a/b enhances mitochondrial glutaminase expression and glutamine metabolism

(2009) Ping Gao et al.   NATURE

HnRNP proteins controlled by c-Myc deregulate pyruvate kinase mRNA splicing in cancer

(2009) Charles J. David et al.   NATURE

Q's next: the diverse functions of glutamine in metabolism, cell biology and cancer

(2009) R J DeBerardinis et al.   ONCOGENE

Lactate Dehydrogenase 5 Expression in Squamous Cell Head and Neck Cancer Relates to Prognosis following Radical or Postoperative Radiotherapy

(2009) Michael I. Koukourakis et al.   ONCOLOGY

Hypoxia stimulates lactate release and modulates monocarboxylate transporter (MCT1, MCT2, and MCT4) expression in human adipocytes

(2009) Fátima Pérez de Heredia et al.   PFLUGERS ARCHIV-EUROPEAN JOURNAL OF PHYSIOLOGY

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

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

Blocking CD147 induces cell death in cancer cells through impairment of glycolytic energy metabolism

(2008) Miyako Baba et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Colon cancer cells maintain low levels of pyruvate to avoid cell death caused by inhibition of HDAC1/HDAC3

(2008) Muthusamy Thangaraju et al.   BIOCHEMICAL JOURNAL

Increasing Expression of Monocarboxylate Transporters 1 and 4 Along Progression to Invasive Cervical Carcinoma

(2008) Céline Pinheiro et al.   INTERNATIONAL JOURNAL OF GYNECOLOGICAL PATHOLOGY

Structural and Biochemical Studies of TIGAR (TP53-induced Glycolysis and Apoptosis Regulator)

(2008) Hua Li et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Targeting lactate-fueled respiration selectively kills hypoxic tumor cells in mice

(2008) Pierre Sonveaux et al.   JOURNAL OF CLINICAL INVESTIGATION

The M2 splice isoform of pyruvate kinase is important for cancer metabolism and tumour growth

(2008) Heather R. Christofk et al.   NATURE

Myc regulates a transcriptional program that stimulates mitochondrial glutaminolysis and leads to glutamine addiction

(2008) D. R. Wise et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Increased expression of monocarboxylate transporters 1, 2, and 4 in colorectal carcinomas

(2008) Céline Pinheiro et al.   VIRCHOWS ARCHIV