Leone RD, Powell JD (2020) Metabolism of immune cells in cancer. Nat Rev Cancer 20:516–531

Article  CAS  PubMed  PubMed Central  Google Scholar 

Gillies RJ, Raghunand N, Karczmar GS et al (2002) MRI of the tumor microenvironment. J Magn Reson Imaging 16:430–450

Article  PubMed  Google Scholar 

Cardone RA, Casavola V, Reshkin SJ (2005) The role of disturbed pH dynamics and the Na+/H+ exchanger in metastasis. Nat Rev Cancer 5:786–795

Article  CAS  PubMed  Google Scholar 

Curtis NJ, Mooney L, Hopcroft L et al (2017) Pre-clinical pharmacology of AZD3965, a selective inhibitor of MCT1: DLBCL, NHL and Burkitt's lymphoma anti-tumor activity. Oncotarget 8:69219–69236

Article  PubMed  PubMed Central  Google Scholar 

Halestrap AP (2012) The monocarboxylate transporter family-structure and functional characterization. IUBMB Life 64:1–9

Article  CAS  PubMed  Google Scholar 

Bosshart PD, Charles RP, Garibsingh RA et al (2021) SLC16 family: from atomic structure to human disease. Trends Biochem Sci 46:28–40

Article  CAS  PubMed  Google Scholar 

Aoi W, Marunaka Y (2014) Importance of pH homeostasis in metabolic health and diseases: crucial role of membrane proton transport. Biomed Res Int 2014:598986

Article  PubMed  PubMed Central  Google Scholar 

Jackson V, Halestrap AJTJ (1996) The kinetics, substrate, and inhibitor specificity of the monocarboxylate (lactate) transporter of rat liver cells determined using the fluorescent intracellular pH indicator, 2',7'-bis(carboxyethyl)-5(6)-carboxyfluorescein. J Biol Chem 271:861–868

Article  CAS  PubMed  Google Scholar 

Bosshart PD, Kalbermatter D, Bonetti S et al (2019) Mechanistic basis of L-lactate transport in the SLC16 solute carrier family. Nat Commun 10:2649

Article  PubMed  PubMed Central  Google Scholar 

Bongarzone S, Barbon E, Ferocino A et al (2020) Imaging niacin trafficking with positron emission tomography reveals in vivo monocarboxylate transporter distribution. Nucl Med Biol 88-89:24–33

Article  CAS  PubMed  PubMed Central  Google Scholar 

Grollman E, Philp N, McPhie P et al (2000) Determination of transport kinetics of chick MCT3 monocarboxylate transporter from retinal pigment epithelium by expression in genetically modified yeast. Biochemistry 39:9351–9357

Article  CAS  PubMed  Google Scholar 

Bonen A (2001) The expression of lactate transporters (MCT1 and MCT4) in heart and muscle. Eur J Appl Physiol 86:6–11

Article  CAS  PubMed  Google Scholar 

Ganapathy V, Thangaraju M, Prasad PD (2009) Nutrient transporters in cancer: relevance to Warburg hypothesis and beyond. Pharmacol Ther 121:29–40

Article  CAS  PubMed  Google Scholar 

Faubert B, Li KY, Cai L et al (2017) Lactate metabolism in human lung tumors. Cell 171(358-371):e359

Google Scholar 

Sonveaux P, Végran F, Schroeder T et al (2008) Targeting lactate-fueled respiration selectively kills hypoxic tumor cells in mice. J Clin Invest

Dimmer KS, Friedrich B, Lang F et al (2000) The low-affinity monocarboxylate transporter MCT4 is adapted to the export of lactate in highly glycolytic cells. Biochem J 350(Pt 1):219–227

Article  CAS  PubMed  PubMed Central  Google Scholar 

Leu M, Kitz J, Pilavakis Y et al (2021) Monocarboxylate transporter-1 (MCT1) protein expression in head and neck cancer affects clinical outcome. Sci Rep 11

Pertega-Gomes N, Vizcaino JR, Miranda-Goncalves V et al (2011) Monocarboxylate transporter 4 (MCT4) and CD147 overexpression is associated with poor prognosis in prostate cancer. BMC Cancer 11:312

Article  PubMed  PubMed Central  Google Scholar 

Afonso J, Pinto T, Simões-Sousa S et al (2019) Clinical significance of metabolism-related biomarkers in non-Hodgkin lymphoma – MCT1 as potential target in diffuse large B cell lymphoma. Cell Oncol 42:303–318

Article  CAS  Google Scholar 

Johnson JM, Cotzia P, Fratamico R et al (2017) MCT1 in invasive ductal carcinoma: monocarboxylate metabolism and aggressive breast cancer. Front Cell Dev Biol 5:27

Article  PubMed  PubMed Central  Google Scholar 

Wang N, Jiang X, Zhang S et al (2021) Structural basis of human monocarboxylate transporter 1 inhibition by anti-cancer drug candidates. Cell 184:370–383.e313

Article  CAS  PubMed  Google Scholar 

Becker HM, Deitmer JW (2020) Transport metabolons and acid/base balance in tumor cells. Cancers 12

Silva A, Antunes B, Batista A et al (2022) In vivo anticancer activity of AZD3965: a systematic review. Molecules 27

Takenaga K, Koshikawa N, Akimoto M et al (2021) MCT4 is induced by metastasis-enhancing pathogenic mitochondrial NADH dehydrogenase gene mutations and can be a therapeutic target. Sci Rep 11:13302

Article  CAS  PubMed  PubMed Central  Google Scholar 

Tateishi H, Tsuji AB, Kato K et al (2017) Synthesis and evaluation of 11C-labeled coumarin analog as an imaging probe for detecting monocarboxylate transporters expression. Bioorg Med Chem Lett 27:4893–4897

Article  CAS  PubMed  Google Scholar 

Draoui N, Schicke O, Fernandes A et al (2013) Synthesis and pharmacological evaluation of carboxycoumarins as a new antitumor treatment targeting lactate transport in cancer cells. Bioorg Med Chem 21:7107–7117

Article  CAS  PubMed  Google Scholar 

Sadeghzadeh M, Moldovan RP, Fischer S et al (2019) Development and radiosynthesis of the first 18F-labeled inhibitor of monocarboxylate transporters (MCTs). J Label Compd Radiopharm 62:411–424

Article  CAS  Google Scholar 

Sattler B, Kranz M, Wenzel B et al (2020) Preclinical incorporation dosimetry of [18F]FACH—a novel 18F-labeled MCT1/MCT4 lactate transporter inhibitor for imaging cancer metabolism with PET. Molecules 25

Sadeghzadeh M, Wenzel B, Gündel D et al (2020) Development of novel analogs of the monocarboxylate transporter ligand FACH and biological validation of one potential radiotracer for positron emission tomography (PET) imaging. Molecules 25

Sadeghzadeh M, Moldovan R-P, Teodoro R et al (2019) One-step radiosynthesis of the MCTs imaging agent [18F]FACH by aliphatic 18F-labelling of a methylsulfonate precursor containing an unprotected carboxylic acid group. Sci Rep 9

Gündel D, Sadeghzadeh M, Deuther-Conrad W et al (2021) Preclinical evaluation of [18F]FACH in healthy mice and piglets: an 18F-labeled ligand for imaging of monocarboxylate transporters with PET. Int J Mol Sci 22

Shimozono M, Scofield MA, Wangemann P (1997) Functional evidence for a monocarboxylate transporter (MCT) in strial marginal cells and molecular evidence for MCT1 and MCT2 in stria vascularis. Hear Res 114:213–222

Article  CAS  PubMed  Google Scholar 

Guan X, Rodriguez-Cruz V, Morris MJTA (2019) 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 21:13

Google Scholar 

Guan X, Bryniarski MA, Morris ME (2018) In vitro and in vivo efficacy of the monocarboxylate transporter 1 inhibitor AR-C155858 in the murine 4T1 breast cancer tumor model. AAPS J 21:3

Article  PubMed  Google Scholar 

Gurrapu S, Jonnalagadda SK, Alam MA et al (2015) Monocarboxylate transporter 1 inhibitors as potential anticancer agents. ACS Med Chem Lett 6:558–561

Article  CAS  PubMed  PubMed Central  Google Scholar 

Odi R, Bibi D, Wager T et al (2020) A perspective on the physicochemical and biopharmaceutic properties of marketed antiseizure drugs—from phenobarbital to cenobamate and beyond. Epilepsia 61:1543–1552

Article  CAS  PubMed  Google Scholar 

Kim D, Ko HY, Chung JI et al (2023) Visualizing cancer-originating acetate uptake through MCT1 in reactive astrocytes in the glioblastoma tumor microenvironment. Neuro-Oncology