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

Cooperative transport mechanism of human monocarboxylate transporter 2

(2020) Bo Zhang et al.   Nature Communications

Structure of the human LAT1–4F2hc heteromeric amino acid transporter complex

(2019) Renhong Yan et al.   NATURE

Serotonin transporter–ibogaine complexes illuminate mechanisms of inhibition and transport

(2019) Jonathan A. Coleman et al.   NATURE

Cryo-EM structure of the human L-type amino acid transporter 1 in complex with glycoprotein CD98hc

(2019) Yongchan Lee et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Mechanistic basis of L-lactate transport in the SLC16 solute carrier family

(2019) Patrick D. Bosshart et al.   Nature Communications

Monocarboxylate transporters in cancer

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

Structure and drug resistance of the Plasmodium falciparum transporter PfCRT

(2019) Jonathan Kim et al.   NATURE

The Science and Translation of Lactate Shuttle Theory

(2018) George A. Brooks   Cell Metabolism

Real-space refinement in PHENIX for cryo-EM and crystallography

(2018) Pavel V. Afonine et al.   Acta Crystallographica Section D-Structural Biology

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

(2018) Maria Quanz et al.   MOLECULAR CANCER THERAPEUTICS

New tools for automated high-resolution cryo-EM structure determination in RELION-3

(2018) Jasenko Zivanov et al.   eLife

MotionCor2: anisotropic correction of beam-induced motion for improved cryo-electron microscopy

(2017) Shawn Q Zheng et al.   NATURE METHODS

cryoSPARC: algorithms for rapid unsupervised cryo-EM structure determination

(2017) Ali Punjani et al.   NATURE METHODS

Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt’s lymphoma anti-tumor activity

(2017) Nicola J. Curtis et al.   Oncotarget

Monocarboxylate transporters in the brain and in cancer

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

Gctf: Real-time CTF determination and correction

(2016) Kai Zhang   JOURNAL OF STRUCTURAL BIOLOGY

Structure of a yeast activated spliceosome at 3.5 A resolution

(2016) C. Yan et al.   SCIENCE

Targeting Metabolic Symbiosis to Overcome Resistance to Anti-angiogenic Therapy

(2016) Laura Pisarsky et al.   Cell Reports

Structural Biology of the Major Facilitator Superfamily Transporters

(2015) Nieng Yan   Annual Review of Biophysics

Identification of key binding site residues of MCT1 for AR-C155858 reveals the molecular basis of its isoform selectivity: Figure 6

(2015) B. Nancolas et al.   BIOCHEMICAL JOURNAL

Monocarboxylate Transporter 1 Deficiency and Ketone Utilization

(2015)   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of Monocarboxylate Transporter-1 (MCT1) by AZD3965 Enhances Radiosensitivity by Reducing Lactate Transport

(2014) B. M. Bola et al.   MOLECULAR CANCER THERAPEUTICS

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

Crystal structure of the human glucose transporter GLUT1

(2014) Dong Deng et al.   NATURE

Structure of malaria invasion protein RH5 with erythrocyte basigin and blocking antibodies

(2014) Katherine E. Wright et al.   NATURE

Structure of the Yeast Mitochondrial Large Ribosomal Subunit

(2014) A. Amunts et al.   SCIENCE

Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells

(2013) Nihed Draoui et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Targeting lactate metabolism for cancer therapeutics

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

The SLC16 gene family – Structure, role and regulation in health and disease

(2013) Andrew P. Halestrap   MOLECULAR ASPECTS OF MEDICINE

Crystal structure of a bacterial homologue of glucose transporters GLUT1–4

(2012) Linfeng Sun et al.   NATURE

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

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

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

The monocarboxylate transporter family-Role and regulation

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

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

I-TASSER: a unified platform for automated protein structure and function prediction

(2010) Ambrish Roy et al.   Nature Protocols

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

Studies on the DIDS-binding Site of Monocarboxylate Transporter 1 Suggest a Homology Model of the Open Conformation and a Plausible Translocation Cycle

(2009) Marieangela C. Wilson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Sodium-coupled Monocarboxylate Transporters in Normal Tissues and in Cancer

(2008) Vadivel Ganapathy et al.   AAPS Journal