Lactate in the tumour microenvironment: From immune modulation to therapy

Metabolic support of tumour-infiltrating regulatory T cells by lactic acid

(2021) McLane J. Watson et al.   NATURE

Cysteine 159 delineates a hinge region of the alternating access monocarboxylate transporter 1 and is targeted by cysteine‐modifying inhibitors

(2021) Anna‐Lena Köpnick et al.   FEBS Journal

Targeting neovascularization and respiration of tumor grafts grown on chick embryo chorioallantoic membranes

(2021) Hyrije Ademi et al.   PLoS One

LDHA induces EMT gene transcription and regulates autophagy to promote the metastasis and tumorigenesis of papillary thyroid carcinoma

(2021) Xiukun Hou et al.   Cell Death & Disease

Inhibition of LDH-A by Oxamate Enhances the Efficacy of Anti-PD-1 Treatment in an NSCLC Humanized Mouse Model

(2021) Tianyun Qiao et al.   Frontiers in Oncology

Phase I expansion study of the first-in-class monocarboxylate transporter 1 (MCT1) inhibitor AZD3965 in patients with diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL).

(2021) Sarah E. R. Halford et al.   JOURNAL OF CLINICAL ONCOLOGY

Transport function, regulation, and biology of human monocarboxylate transporter 1 (hMCT1) and 4 (hMCT4)

(2021) Masaki Kobayashi et al.   PHARMACOLOGY & THERAPEUTICS

Impaired lipid biosynthesis hinders anti-tumor efficacy of intratumoral iNKT cells

(2020) Sicheng Fu et al.   Nature Communications

Lactic Acidosis Together with GM-CSF and M-CSF Induces Human Macrophages toward an Inflammatory Protumor Phenotype

(2020) Léa Paolini et al.   Cancer Immunology Research

Inhibition of Alternative Cancer Cell Metabolism of EGFR Mutated Non-Small Cell Lung Cancer Serves as a Potential Therapeutic Strategy

(2020) Chung-Yu Huang et al.   Cancers

Tumor‐Targeted Inhibition of Monocarboxylate Transporter 1 Improves T‐Cell Immunotherapy of Solid Tumors

(2020) Tongyi Huang et al.   Advanced Healthcare Materials

Extracellular Acidosis and mTOR Inhibition Drive the Differentiation of Human Monocyte-Derived Dendritic Cells

(2020) Fernando Erra Díaz et al.   Cell Reports

Lactate Increases Renal Cell Carcinoma Aggressiveness through Sirtuin 1-Dependent Epithelial Mesenchymal Transition Axis Regulation

(2020) Vera Miranda-Gonçalves et al.   Cells

Synergisms of genome and metabolism stabilizing antitumor therapy (GMSAT) in human breast and colon cancer cell lines: a novel approach to screen for synergism

(2020) Jérôme Ruhnau et al.   BMC CANCER

Impact of hypoxia on chemoresistance of mesothelioma mediated by the proton-coupled folate transporter, and preclinical activity of new anti-LDH-A compounds

(2020) Giovanna Li Petri et al.   BRITISH JOURNAL OF CANCER

Metformin and Everolimus: A Promising Combination for Neuroendocrine Tumors Treatment

(2020) Eleonora Vitali et al.   Cancers

AT101-Loaded Cubosomes as an Alternative for Improved Glioblastoma Therapy

(2020) Dorota K Flak et al.   International Journal of Nanomedicine

Targeting lactate dehydrogenase A ( LDHA ) exerts antileukemic effects on T‐cell acute lymphoblastic leukemia

(2020) Haizhi Yu et al.   Cancer Communications

Oncometabolites lactate and succinate drive pro-angiogenic macrophage response in tumors

(2020) Marjolein M.G. Kes et al.   BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER

Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates

(2020) Nan Wang et al.   CELL

Metformin induced lactic acidosis impaired response of cancer cells towards paclitaxel and doxorubicin: Role of monocarboxylate transporter

(2020) Shivendra Vikram Singh et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR BASIS OF DISEASE

Cellular Uptake of MCT1 Inhibitors AR-C155858 and AZD3965 and Their Effects on MCT-Mediated Transport of L-Lactate in Murine 4T1 Breast Tumor Cancer Cells

(2019) Xiaowen Guan et al.   AAPS Journal

Lactate modulates CD4+ T-cell polarization and induces an immunosuppressive environment, which sustains prostate carcinoma progression via TLR8/miR21 axis

(2019) G. Comito et al.   ONCOGENE

Hypoxia/pseudohypoxia‐mediated activation of hypoxia‐inducible factor‐1α in cancer

(2019) Yoshihiro Hayashi et al.   CANCER SCIENCE

Microenvironmental Metabolism Regulates Antitumor Immunity

(2019) Verra M. Ngwa et al.   CANCER RESEARCH

Targeting mTOR for cancer therapy

(2019) Hui Hua et al.   Journal of Hematology & Oncology

Monocarboxylate transporters in cancer

(2019) Valéry L. Payen et al.   Molecular Metabolism

Lactate Induces Pro-tumor Reprogramming in Intratumoral Plasmacytoid Dendritic Cells

(2019) Deblina Raychaudhuri et al.   Frontiers in Immunology

Targeting Pyruvate Kinase M2 and Lactate Dehydrogenase A Is an Effective Combination Strategy for the Treatment of Pancreatic Cancer

(2019) Goran Hamid Mohammad et al.   Cancers

Metabolic regulation of gene expression by histone lactylation

(2019) Di Zhang et al.   NATURE

Restricting Glycolysis Preserves T Cell Effector Functions and Augments Checkpoint Therapy

(2019) Kathrin Renner et al.   Cell Reports

Lactate Buildup at the Site of Chronic Inflammation Promotes Disease by Inducing CD4+ T Cell Metabolic Rewiring

(2019) Valentina Pucino et al.   Cell Metabolism

Lactate/GPR81 signaling and proton motive force in cancer: Role in angiogenesis, immune escape, nutrition, and Warburg phenomenon

(2019) Timothy P. Brown et al.   PHARMACOLOGY & THERAPEUTICS

Acid Suspends the Circadian Clock in Hypoxia through Inhibition of mTOR

(2018) Zandra E. Walton et al.   CELL

The Science and Translation of Lactate Shuttle Theory

(2018) George A. Brooks   Cell Metabolism

Oxidative Phosphorylation as an Emerging Target in Cancer Therapy

(2018) Thomas M. Ashton et al.   CLINICAL CANCER RESEARCH

Lactate metabolism: historical context, prior misinterpretations, and current understanding

(2018) Brian S. Ferguson et al.   EUROPEAN JOURNAL OF APPLIED PHYSIOLOGY

Interruption of lactate uptake by inhibiting mitochondrial pyruvate transport unravels direct antitumor and radiosensitizing effects

(2018) Cyril Corbet et al.   Nature Communications

The Monocarboxylate transporter inhibitor Quercetin induces intracellular acidification in a mouse model of Glioblastoma Multiforme: in-vivo detection using magnetic resonance imaging

(2018) Mohammed Albatany et al.   INVESTIGATIONAL NEW DRUGS

Double genetic disruption of lactate dehydrogenase A and B is required to ablate the ‘Warburg effect’ restricting tumor growth to oxidative metabolism

(2018) Maša Ždralević et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Preclinical Efficacy of the Novel Monocarboxylate Transporter 1 Inhibitor BAY-8002 and Associated Markers of Resistance

(2018) Maria Quanz et al.   MOLECULAR CANCER THERAPEUTICS

Lactate inhibits ATP6V0d2 expression in tumor-associated macrophages to promote HIF-2α–mediated tumor progression

(2018) Na Liu et al.   JOURNAL OF CLINICAL INVESTIGATION

Lactate dehydrogenase A: A key player in carcinogenesis and potential target in cancer therapy

(2018) Yangbo Feng et al.   Cancer Medicine

Lactate: A Metabolic Driver in the Tumour Landscape

(2018) Luigi Ippolito et al.   TRENDS IN BIOCHEMICAL SCIENCES

Programmed cell death-1 (PD-1) checkpoint blockade in combination with a mammalian target of rapamycin inhibitor restrains hepatocellular carcinoma growth induced by hepatoma cell-intrinsic PD-1

(2017) Hui Li et al.   HEPATOLOGY

Glucose feeds the TCA cycle via circulating lactate

(2017) Sheng Hui et al.   NATURE

Lactic Acid: No Longer an Inert and End-Product of Glycolysis

(2017) Shiren Sun et al.   PHYSIOLOGY

Gpr132 sensing of lactate mediates tumor–macrophage interplay to promote breast cancer metastasis

(2017) Peiwen Chen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Targeting pH regulating proteins for cancer therapy–Progress and limitations

(2017) Scott K. Parks et al.   SEMINARS IN CANCER BIOLOGY

Metabolic coupling and the Reverse Warburg Effect in cancer: Implications for novel biomarker and anticancer agent development

(2017) Lindsay Wilde et al.   SEMINARS IN ONCOLOGY

Intracellular Hyper-Acidification Potentiated by Hydrogen Sulfide Mediates Invasive and Therapy Resistant Cancer Cell Death

(2017) Zheng-Wei Lee et al.   Frontiers in Pharmacology

The anti-tumour agent lonidamine is a potent inhibitor of the mitochondrial pyruvate carrier and plasma membrane monocarboxylate transporters

(2016) B. Nancolas et al.   BIOCHEMICAL JOURNAL

Monocarboxylate transporters in the brain and in cancer

(2016) Jhudit Pérez-Escuredo et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Metabolic Heterogeneity in Human Lung Tumors

(2016) Christopher T. Hensley et al.   CELL

LDHA-Associated Lactic Acid Production Blunts Tumor Immunosurveillance by T and NK Cells

(2016) Almut Brand et al.   Cell Metabolism

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition

(2016) Aaron Boudreau et al.   Nature Chemical Biology

Lactic acid in tumor microenvironments causes dysfunction of NKT cells by interfering with mTOR signaling

(2016) Di Xie et al.   Science China-Life Sciences

Monocarboxylate transport inhibition potentiates the cytotoxic effect of 5-fluorouracil in colorectal cancer cells

(2015) Ricardo Amorim et al.   CANCER LETTERS

Oxamate-mediated inhibition of lactate dehydrogenase induces protective autophagy in gastric cancer cells: Involvement of the Akt–mTOR signaling pathway

(2015) Zhi Zhao et al.   CANCER LETTERS

Amino Acid Transporters in Cancer and Their Relevance to "Glutamine Addiction": Novel Targets for the Design of a New Class of Anticancer Drugs

(2015) Y. D. Bhutia et al.   CANCER RESEARCH

Recent Update on Human Lactate Dehydrogenase Enzyme 5 (hLDH5) Inhibitors: A Promising Approach for Cancer Chemotherapy

(2015) Reshma Rani et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Phase I Trial of DFMO Targeting Polyamine Addiction in Patients with Relapsed/Refractory Neuroblastoma

(2015) Giselle L. Saulnier Sholler et al.   PLoS One

Lactate Regulates Metabolic and Pro-inflammatory Circuits in Control of T Cell Migration and Effector Functions

(2015) Robert Haas et al.   PLOS BIOLOGY

HIF-1α pathway: role, regulation and intervention for cancer therapy

(2015) Georgina N. Masoud et al.   Acta Pharmaceutica Sinica B

Antitumor Activity of 7-Aminocarboxycoumarin Derivatives, a New Class of Potent Inhibitors of Lactate Influx but Not Efflux

(2014) N. Draoui et al.   MOLECULAR CANCER THERAPEUTICS

Catabolic cancer-associated fibroblasts transfer energy and biomass to anabolic cancer cells, fueling tumor growth

(2014) Ubaldo E. Martinez-Outschoorn et al.   SEMINARS IN CANCER BIOLOGY

Synergistic interaction of novel lactate dehydrogenase inhibitors with gemcitabine against pancreatic cancer cells in hypoxia

(2013) M Maftouh et al.   BRITISH JOURNAL OF CANCER

Downregulation of MCT1 inhibits tumor growth, metastasis and enhances chemotherapeutic efficacy in osteosarcoma through regulation of the NF-κB pathway

(2013) Zhiqiang Zhao et al.   CANCER LETTERS

Activity of the Monocarboxylate Transporter 1 Inhibitor AZD3965 in Small Cell Lung Cancer

(2013) R. Polanski et al.   CLINICAL CANCER RESEARCH

Targeting lactate metabolism for cancer therapeutics

(2013) Joanne R. Doherty et al.   JOURNAL OF CLINICAL INVESTIGATION

Phosphofructokinase deficiency impairs ATP generation, autophagy, and redox balance in rheumatoid arthritis T cells

(2013) Zhen Yang et al.   JOURNAL OF EXPERIMENTAL MEDICINE

Dendritic Cell Reprogramming by Endogenously Produced Lactic Acid

(2013) A. Nasi et al.   JOURNAL OF IMMUNOLOGY

Tumor-derived lactate and myeloid-derived suppressor cells: Linking metabolism to cancer immunology

(2013) Zaheed Husain et al.   OncoImmunology

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

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

Lactate, a product of glycolytic metabolism, inhibits histone deacetylase activity and promotes changes in gene expression

(2012) Tom Latham et al.   NUCLEIC ACIDS RESEARCH

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

(2011) Hiroto Izumi et al.   CANCER SCIENCE

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

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

Therapeutic targeting of cancer cell metabolism

(2011) Chi V. Dang et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Mammalian target of rapamycin up-regulation of pyruvate kinase isoenzyme type M2 is critical for aerobic glycolysis and tumor growth

(2011) Q. Sun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Differential activation and antagonistic function of HIF-  isoforms in macrophages are essential for NO homeostasis

(2010) N. Takeda et al.   GENES & DEVELOPMENT

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

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

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

Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth

(2008) B. Clem et al.   MOLECULAR CANCER THERAPEUTICS

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