z Abid SH, Malhotra V, Perry MC (2001) Radiation-induced and
chemotherapy-induced pulmonary injury. Curr Opin Oncol 13:242-8.
https://doi.org/10.1097/00001622-200107000-00006
z Batlle E, Sancho E, Francí C, et al. (2000) The transcription factor snail
is a repressor of E-cadherin gene expression in epithelial tumour
cells. Nat Cell Biol 2:84-89. https://doi:10.1038/35000034
z Benedek TG (2010) Methotrexate: from its introduction to non-
oncologic therapeutics to anti-TNF-α. Clin Exp Rheumatol 28 (5 Suppl
61):S3-S8.
z Bergersen LH (2007) Is lactate food for neurons? Comparison of
monocarboxylate transporter subtypes in brain and muscle.
Neuroscience 145:11-19.
https://doi:10.1016/j.neuroscience.2006.11.062
z Bleyer WA (1978) The clinical pharmacology of methotrexate: new
applications of an old drug. Cancer 41:36-51.
https://doi:10.1002/1097-0142(197801)41:1<36::aidcncr2820410108>3.0.co;2-i
80
z Bröer S, Bröer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW
(1999) Characterization of the high-affinity monocarboxylate
transporter MCT2 in Xenopus laevis oocytes. Biochem J 341:529–
535. https://doi.org/10.1042/0264-6021:3410529
z Brooks GA. Cell-cell and intracellular lactate shuttles (2009) J Physiol
587:5591-5600. https://doi:10.1113/jphysiol.2009.178350
z Cano A, Pérez-Moreno MA, Rodrigo I, et al. (2000) The transcription
factor snail controls epithelial-mesenchymal transitions by
repressing E-cadherin expression. Nat Cell Biol 2(2):76-83.
https://doi:10.1038/35000025
z Choi JW, Kim Y, Lee JH, Kim YS (2014) Prognostic significance of
lactate/proton symporters MCT1, MCT4, and their chaperone
CD147 expressions in urothelial carcinoma of the bladder. Urology
84:245.e9-15. https://doi.org/10.1016/j.urology.2014.03.031
z DeBerardinis RJ, Lum JJ, Hatzivassiliou G, Thompson CB (2008) The
biology of cancer: metabolic reprogramming fuels cell growth and
proliferation. Cell Metab 7:11–20.
https://doi.org/10.1016/j.cmet.2007.10.002
81
z Deuticke B (1982) Monocarboxylate transport in erythrocytes. J
Membr Biol 70:89-103. https://doi:10.1007/BF01870219
z Doherty JR, Yang C, Scott KE, et al. (2014) Blocking lactate export by
inhibiting the Myc target MCT1 Disables glycolysis and glutathione
synthesis. Cancer Res 74:908–920.
https://doi.org/10.1158/00085472.CAN-13-2034
z Eilertsen M, Andersen S, Al-Saad S et al. (2014) Monocarboxylate
transporters 1-4 in NSCLC: MCT1 is an independent prognostic
marker for survival. PLoS One 9:e105038.
https://doi.org/10.1371/journal.pone.0105038
z Fang J, Quinones QJ, Holman TL, et al. (2006) The H+-linked
monocarboxylate transporter (MCT1/SLC16A1): a potential
therapeutic target for high-risk neuroblastoma. Mol Pharmacol
70:2108–2115. https://doi.org/10.1124/mol.106.026245
z Feron O (2009) Pyruvate into lactate and back: from the Warburg
effect to symbiotic energy fuel exchange in cancer cells. Radiother
Oncol 92:329–333. https://doi.org/10.1016/j.radonc.2009.06.025
82
z Fiaschi T, Marini A, Giannoni E, et al. (2012) Reciprocal metabolic
reprogramming through lactate shuttle coordinately influences
tumor-stroma interplay. Cancer Res 72:5130–5140.
https://doi.org/10.1158/0008-5472.CAN-12-1949
z Fishbein WN, Merezhinskaya N, Foellmer JW (2002) Relative
distribution of three major lactate transporters in frozen human
tissues and their localization in unfixed skeletal muscle. Muscle
Nerve 26:101–112. https://doi.org/10.1002/mus.10168
z Gan L, Xiu R, Ren P, et al. (2016) Metabolic targeting of oncogene
MYC by selective activation of the proton-coupled
monocarboxylate family of transporters. Oncogene 35(23):30373048. https://doi:10.1038/onc.2015.360
z Garcia CK, Goldstein JL, Pathak RK, Anderson RG, Brown MS (1994)
Molecular characterization of a membrane transporter for lactate,
pyruvate, and other monocarboxylates: implications for the Cori
cycle. Cell 76:865–873. https://doi.org/10.1016/00928674(94)90361-1
83
z Gray AL, Coleman DT, Shi R, Cardelli JA (2016) Monocarboxylate
transporter 1 contributes to growth factor-induced tumor cell
migration independent of transporter activity. Oncotarget 7:32695–
32706. https://doi.org/10.18632/oncotarget.9016
z Halestrap AP, Denton RM (1974) Specific inhibition of pyruvate
transport in rat liver mitochondria and human erythrocytes by
acyano-4-hydroxycinnamate. Biochem J 138:313–316.
https://doi.org/10.1042/bj1380313
z Halestrap AP, Meredith D (2004) The SLC16 gene family-from
monocarboxylate transporters (MCTs) to aromatic amino acid
transporters and beyond. Pflugers Arch 447:619–628.
https://doi.org/10.1007/s00424-003-1067-2
z Halestrap AP, Price NT (1999) The proton-linked monocarboxylate
transporter (MCT) family: structure, function and regulation.
Biochem J 343:281-299.
z Halestrap AP, Wilson MC (2012) The monocarboxylate transporter
family–role and regulation. IUBMB Life 64:109–119.
https://doi.org/10.1002/iub.572
84
z Ikehata M, Yumoto R, Nakamura K, Nagai J, Takano M (2008)
Comparison of albumin uptake in rat alveolar type II and type I-like
epithelial cells in primary culture. Pharm Res 25:913-922.
https://doi:10.1007/s11095-007-9426-x
z Kalluri R, Neilson EG (2003) Epithelial-mesenchymal transition and
its implications for fibrosis. J Clin Invest 112:1776–1784. https://doi.
org/10.1172/JCI20530
z Kalluri R, Weinberg RA (2009) The basics of epithelial-mesenchymal
transition. J Clin Invest 119:1420–1428.
https://doi.org/10.1172/JCI39104
z Kang H, Kim H, Lee S et al. (2019) Role of metabolic reprogramming
in epithelial–mesenchymal transition (EMT). Int J Mol Sci 20:2042.
https://doi.org/10.3390/ijms20082042
z Kawami M, Deguchi J, Yumoto R, Sakakibara N, Tsukamoto I, Konishi
R, Takano M (2017) Effect of COA-Cl on transforming growth factor-
β1-induced epithelial-mesenchymal transition in RLE/Abca3 cells.
Drug Metab Pharmacokinet 32:224–227.
https://doi.org/10.1016/j.dmpk.2017.05.001
85
z Kawami M, Harabayashi R, Harada R, Yamagami Y, Yumoto R, Takano
M(2018) Folic acid prevents methotrexate-induced epithelial
mesenchymal transition via suppression of secreted factors from the
human alveolar epithelial cell line A549. Biochem Biophys Res
Commun 497:457–463. https://doi.org/10.1016/j.bbrc.2018.02.111
z Kawami M, Harabayashi R, MiyamotoM, Harada R, Yumoto R, Takano
M (2016) Methotrexate-induced epithelial–mesenchymal transition in
the alveolar epithelial cell line A549. Lung 194:923–930.
https://doi.org/10.1007/s00408-016-9935-7
z Kawami M, Yamada Y, Issarachot O, Junyaprasert VB, Yumoto R, Takano
M (2018) P-gp modulating effect of Azadirachta indica extract in
multidrug-resistant cancer cell lines. Pharmazie 73:104–109.
https://doi.org/10.1691/ph.2018.7116
z Kim KK, Kugler MC, Wolters PJ et al. (2006) Alveolar epithelial cell
mesenchymal transition develops in vivo during pulmonary fibrosis
and is regulated by the extracellular matrix. Proc Natl Acad Sci USA
103:13180–13185. https://doi.org/10.1073/pnas.0605669103
86
z Koppenol WH, Bounds PL, Dang CV (2011) Otto Warburg’s
contributions to current concepts of cancer metabolism. Nat Rev
Cancer 11:325–337. https://doi.org/10.1038/nrc3038
z Kottmann RM, Hogan CM, Phipps RP, Sime PJ (2009) Determinants of
initiation and progression of idiopathic pulmonary
fibrosis. Respirology 14:917-933. https://doi:10.1111/j.14401843.2009.01624.x
z Kottmann RM, Kulkarni AA, Smolnycki KA, et al. (2012) Lactic acid is
elevated in idiopathic pulmonary fibrosis and induces myofibroblast
differentiation via pH-dependent activation of transforming growth
factor-β. Am J Respir Crit Care Med 186:740–751.
https://doi.org/10.1164/rccm.201201-0084OC
z Lieber M, Smith B, Szakal A et al (1976) A continuous tumor-cell line
from a human lung carcinoma with properties of type II alveolar
epithelial cells. Int J Cancer 17:62–70.
https://doi.org/10.1002/ijc.2910170110
z Liu M, Quek LE, Sultani G, Turner N (2016) Epithelial-mesenchymal
transition induction is associated with augmented glucose uptake
and lactate production in pancreatic ductal adenocarcinoma. Cancer
Metab 4:19. https://doi.org/10.1186/s40170-016-0160-x
87
z Lottes RG, Newton DA, Spyropoulos DD, Baatz JE (2014) Alveolar type
II cells maintain bioenergetic homeostasis in hypoxia through
metabolic and molecular adaptation. Am J Physiol Lung Cell Mol
Physiol 306:L947–L955. https://doi.org/10.1152/ajplung.00298.2013
z Lottes RG, Newton DA, Spyropoulos DD, Baatz JE (2015) Lactate as
substrate for mitochondrial respiration in alveolar epithelial type II
cells. Am J Physiol Lung CellMol Physiol 308:L953–L961.
https://doi.org/10.1152/ajplung.00335.2014
z Martinez FJ, Safrin S, Weycker D, et al. (2005) The clinical course of
patients with idiopathic pulmonary fibrosis. Ann Intern Med 142:963967. https://doi.org/10.7326/0003-4819-142-12_part_1-20050621000005
z Morais-Santos F, Granja S, Miranda-Gonçalves V, et al. (2015)
Targeting lactate transport suppresses in vivo breast tumour growth.
Oncotarget 6:19177–19189.
https://doi.org/10.18632/oncotarget.3910
z Morandi A, Taddei ML, Chiarugi P, Giannoni E (2017) Targeting the
metabolic reprogramming that controls epithelial-to-mesenchymal
transition in aggressive tumors. Front Oncol 7:40.
https://doi.org/10.3389/fonc.2017.00040
88
z Morris ME, Felmlee MA (2008) Overview of the proton-coupled MCT
(SLC16A) family of transporters: characterization, function and role in
the transport of the drug of abuse gamma-hydroxybutyric acid. AAPS J
10:311-321. https://doi:10.1208/s12248-008-9035-6
z Nieto MA, Huang RY, Jackson RA, Thiery JP (2016) EMT:2016. Cell
166:21-45. https://doi:10.1016/j.cell.2016.06.028
z Ohbayashi M, Kubota S, Kawase A, Kohyama N, Kobayashi Y,
Yamamoto T (2014) Involvement of epithelial-mesenchymal transition
in methotrexate-induced pulmonary fibrosis. J Toxicol Sci 39:319-330.
https://doi.org/10.2131/jts.39.319
z Onder TT, Gupta PB, Mani SA, Yang J, Lander ES, Weinberg RA (2008)
Loss of E-cadherin promotes metastasis via multiple downstream
transcriptional pathways. Cancer Res. 68:3645-3654.
https://doi:10.1158/0008-5472.CAN-07-2938
z Ovens MJ, Davies AJ, Wilson MC, Murray CM, Halestrap AP (2010) ARC155858 is a potent inhibitor of monocarboxylate transporters MCT1
and MCT2 that binds to an intracellular site involving transmembrane
helices 7-10. Biochem J 425:523-530. https://doi:10.1042/BJ20091515
89
z Peinado H, Olmeda D, Cano A (2007) Snail Zeb and bHLH factors in
tumour progression: an alliance against the epithelial phenotype?
Nat Rev Cancer 7:415-428. https://doi:10.1038/nrc2131
z Poole RC, Halestrap AP (1993) Transport of lactate and other
monocarboxylates across mammalian plasma membranes. Am J
Physiol 264:C761– C782.
https://doi.org/10.1152/ajpcell.1993.264.4.C761
z Poole RC, Halestrap AP (1994) N-Terminal protein sequence analysis
of the rabbit erythrocyte lactate transporter suggests identity with
the cloned monocarboxylate transport protein MCT1. Biochem J 303:
755–759. https://doi.org/10.1042/bj3030755
z Rajitha P, Biswas R, Sabitha M, Jayakumar R (2017) Methotrexate in
the treatment of psoriasis and rheumatoid arthritis: mechanistic
insights, current issues and novel delivery approaches. Curr Pharm
Des 23:3550-3566.
https://doi.org/10.2174/1381612823666170601105439
z Raghu G, Weycker D, Edelsberg J, Bradford WZ, Oster G (2006)
Incidence and prevalence of idiopathic pulmonary fibrosis. Am J
Respir Crit Care Med 174:810-816.
https://doi.org/10.1164/rccm.200602-163OC
90
z Shi M, Zhu J, Wang R, et al. (2011) Latent TGF-β structure and
activation. Nature 474:343–349.
https://doi.org/10.1038/nature10152
z Smith AP, Verrecchia A, Fagà G, et al (2009) A positive role for Myc
in TGFbeta-induced Snail transcription and epithelial-tomesenchymal transition. Oncogene 28(3):422-430.
https://doi:10.1038/onc.2008.395
z Thorens B, Mueckler M (2010) Glucose transporters in the 21st
Century. Am J Physiol Endocrinol Metab 298:E141-E145.
https://doi.org/10.1152/ajpendo.00712.2009
z Takano M, Yamamoto C, Yamaguchi K et al. (2015) Analysis of TGFβ1-and drug-induced epithelial-mesenchymal transition in cultured
alveolar epithelial cell line RLE/Abca3. Drug Metab Pharmacokint
30:111–118. https://doi.org/10.1016/j.dmpk.2014.10.007
z Thorens B (1996) Glucose transporters in the regulation of intestinal,
renal, and liver glucose fluxes. Am J Physiol. 270:G541-G553.
https://doi.org/10.1152/ajpgi.1996.270.4.G541
91
z Thorens B, Mueckler M (2010) Glucose transporters in the 21st
Century. Am J Physiol Endocrinol Metab 298: E141-5.
https://doi.org/10.1152/ajpendo.00712.2009
z Tuder RM, Lara AR, Thannickal VJ (2012) Lactate, a novel trigger of
transforming growth factor-β activation in idiopathic pulmonary
fibrosis. Am J Respir Crit Care Med 186:701–70.
https://doi.org/10.1164/rccm.201208-1491ED
z Valvona CJ, Fillmore HL, Nunn PB, Pilkington GJ (2016) The Regulation
and Function of Lactate Dehydrogenase A: Therapeutic Potential in
Brain Tumor. Brain Pathol 26:3-17. https://doi:10.1111/bpa.12299
z Willis BC, Borok Z (2007) TGF-β-induced EMT: mechanisms and
implications for fibrotic lung disease. Am J Physiol Lung Cell Mol
Physiol 293:L535–L534. https://doi.org/10.1152/ajplung.00163
z Wolters PJ, Collard HR, Jones KD (2014) Pathogenesis of idiopathic
pulmonary fibrosis. Annu Rev Pathol 9:157–179.
https://doi.org/10.1146/annurev-pathol-012513-104706
z Wynn TA (2008) Cellular and molecular mechanisms of fibrosis. J
Pathol 214:199-210. https://doi.org/10.1002/path.2277
92
z Xie N, Tan Z, Banerjee S, et al. (2015) Glycolytic Reprogramming in
Myofibroblast Differentiation and Lung Fibrosis. Am J Respir Crit
Care Med 192:1462–1474. https://doi.org/10.1164/rccm.2015040780OC
z Yu K, Li Q, Shi G, Li N (2018) Involvement of epithelial-mesenchymal
transition in liver fibrosis. Saudi J Gastroenterol 24:5-11.
https://doi.org/10.4103/sjg.SJG_297_17
z Zank DC, Bueno M, Mora AL, Rojas M (2018) Idiopathic pulmonary
fibrosis: aging, mitochondrial dysfunction, and cellular
bioenergetics. Front Med 5:10.
https://doi.org/10.3389/fmed.2018.00010
z Zhang G, Zhang Y, Dong D, et al. (2018) MCT1 regulates aggressive
and metabolic phenotypes in bladder cancer. J Cancer 9:2492–2501.
https://doi.org/10.7150/jca.25257
93
...