[1] STACPOOLE P W. The dichloroacetate dilemma: environmental hazard versus therapeutic goldmine: both or neither? [J]. Environ Health Perspect, 2011, 119(2): 155-158.
[2] JAMES M O, JAHN S C, ZHONG G, et al. Therapeutic applications of dichloroacetate and the role of glutathione transferase Zeta-1[J]. Pharmacol Ther,2017,170:166-180. doi:  10.1016/j.pharmthera.2016.10.018
[3] MOORE G W, SWIFT L L, RABINOWITZ D, et al. Reduction of serum cholesterol in two patients with homozygous familial hypercholesterolemia by dichloroacetate[J]. Atherosclerosis,1979,33(3):285-293. doi:  10.1016/0021-9150(79)90180-1
[4] IARC Working Group on the Evaluation of Carcinogenic Risks to Humans. Trichloroethylene, tetrachloroethylene, and some other chlorinated agents[S]. IARC Monogr Eval Carcinog Risks Hum, 2014, 106: 1-512.
[5] TATARANNI T, PICCOLI C. Dichloroacetate (DCA) and cancer: an overview towards clinical applications[J]. Oxid Med Cell Longev,2019,2019:8201079.
[6] STAKIŠAITIS D, JUKNEVIČIENĖ M, DAMANSKIENĖ E, et al. The importance of gender-related anticancer research on mitochondrial regulator sodium dichloroacetate in preclinical studies in vivo[J]. Cancers,2019,11(8):1210. doi:  10.3390/cancers11081210
[7] KATO M, LI J, CHUANG J L, et al. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol[J]. Structure,2007,15(8):992-1004. doi:  10.1016/j.str.2007.07.001
[8] EL-HATTAB A W, ZARANTE A M, ALMANNAI M, et al. Therapies for mitochondrial diseases and current clinical trials[J]. Mol Genet Metab,2017,122(3):1-9. doi:  10.1016/j.ymgme.2017.09.009
[9] STACPOOLE P W. The pyruvate dehydrogenase complex as a therapeutic target for age-related diseases[J]. Aging Cell,2012,11(3):371-377. doi:  10.1111/j.1474-9726.2012.00805.x
[10] STACPOOLE P W, MOORE G W, KORNHAUSER D M. Metabolic effects of dichloroacetate in patients with diabetes mellitus and hyperlipoproteinemia[J]. N Engl J Med,1978,298(10):526-530. doi:  10.1056/NEJM197803092981002
[11] STACPOOLE P W, BRIDGE D M, ALVAREZ I M, et al. In vivo regulation of human mononuclear leukocyte 3-hydroxy-3-methylglutaryl coenzyme A reductase. Decreased enzyme catalytic efficiency in familial hypercholesterolemia[J]. J Clin Invest,1987,80(5):1401-1408. doi:  10.1172/JCI113218
[12] SHANGRAW R E, WINTER R, HROMCO J, et al. Amelioration of lactic acidosis with dichloroacetate during liver transplantation in humans[J]. Anesthesiology,1994,81(5):1127-1138. doi:  10.1097/00000542-199411000-00006
[13] ABDELMALAK M, LEW A, RAMEZANI R, et al. Long-term safety of dichloroacetate in congenital lactic acidosis[J]. Mol Genet Metab,2013,109(2):139-143. doi:  10.1016/j.ymgme.2013.03.019
[14] STACPOOLE P W, GILBERT L R, NEIBERGER R E, et al. Evaluation of long-term treatment of children with congenital lactic acidosis with dichloroacetate[J]. Pediatrics,2008,121(5):e1223-e1228. doi:  10.1542/peds.2007-2062
[15] STACPOOLE P W, LORENZ A C, THOMAS R G, et al. Dichloroacetate in the treatment of lactic acidosis[J]. Ann Intern Med,1988,108(1):58-63. doi:  10.7326/0003-4819-108-1-58
[16] STACPOOLE P W, WRIGHT E C, BAUMGARTNER T G, et al. A controlled clinical trial of dichloroacetate for treatment of lactic acidosis in adults[J]. N Engl J Med,1992,327(22):1564-1569. doi:  10.1056/NEJM199211263272204
[17] ANSELM I A, DARRAS B T. Dichloroacetate causes toxic neuropathy in MELAS: a randomized, controlled clinical trial[J]. Neurology, 2006, 67(7): 1313; authorreply1313.
[18] ANDREASSEN O A, FERRANTE R J, HUANG H M, et al. Dichloroacetate exerts therapeutic effects in transgenic mouse models of Huntington’s disease[J]. Ann Neurol,2001,50(1):112-117. doi:  10.1002/ana.1085
[19] PEELING J, SUTHERLAND G, BROWN R A, et al. Protective effect of dichloroacetate in a rat model of forebrain ischemia[J]. Neurosci Lett,1996,208(1):21-24. doi:  10.1016/0304-3940(96)12542-8
[20] GOODMAN J C, ROBERTSON C S, GROSSMAN R G, et al. Elevation of tumor necrosis factor in head injury[J]. J Neuroimmunol,1990,30(2-3):213-217. doi:  10.1016/0165-5728(90)90105-V
[21] KANKOTIA S, STACPOOLE P W. Dichloroacetate and cancer: new home for an orphan drug? [J]. Biochim Biophys Acta, 2014, 1846(2): 617-629.
[22] JAMES M O, STACPOOLE P W. Pharmacogenetic considerations with dichloroacetate dosing[J]. Pharmacogenomics,2016,17(7):743-753. doi:  10.2217/pgs-2015-0012
[23] DUNBAR E M, COATS B S, SHROADS A L, et al. Phase 1 trial of dichloroacetate (DCA) in adults with recurrent malignant brain tumors[J]. Invest New Drugs,2014,32(3):452-464. doi:  10.1007/s10637-013-0047-4
[24] SUTENDRA G, BONNET S, ROCHEFORT G, et al. Fatty acid oxidation and malonyl-CoA decarboxylase in the vascular remodeling of pulmonary hypertension[J]. Sci Transl Med,2010,2(44):44ra58.
[25] CHU Q S C, SANGHA R, SPRATLIN J, et al. A phase I open-labeled, single-arm, dose-escalation, study of dichloroacetate (DCA) in patients with advanced solid tumors[J]. Investig New Drugs,2015,33(3):603-610. doi:  10.1007/s10637-015-0221-y
[26] GARON E B, CHRISTOFK H R, HOSMER W, et al. Dichloroacetate should be considered with platinum-based chemotherapy in hypoxic tumors rather than as a single agent in advanced non-small cell lung cancer[J]. J Cancer Res Clin Oncol,2014,140(3):443-452. doi:  10.1007/s00432-014-1583-9
[27] ZHANG W, ZHANG S L, HU X, et al. Targeting tumor metabolism for cancer treatment: is pyruvate dehydrogenase kinases (PDKs) a viable anticancer target? [J]. Int J Biol Sci, 2015, 11(12): 1390-1400.
[28] STRUM S B, ADALSTEINSSON O, BLACK R R, et al. Case report: Sodium dichloroacetate (DCA) inhibition of the “Warburg Effect” in a human cancer patient: complete response in non-Hodgkin's lymphoma after disease progression with rituximab-CHOP[J]. J Bioenerg Biomembr,2013,45(3):307-315. doi:  10.1007/s10863-012-9496-2
[29] GERRIETS V A, DANZAKI K, KISHTON R J, et al. Leptin directly promotes T-cell glycolytic metabolism to drive effector T-cell differentiation in a mouse model of autoimmunity[J]. Eur J Immunol,2016,46(8):1970-1983. doi:  10.1002/eji.201545861
[30] OSTROUKHOVA M, GOPLEN N, KARIM M Z, et al. The role of low-level lactate production in airway inflammation in asthma[J]. Am J Physiol Lung Cell Mol Physiol,2012,302(3):L300-L307. doi:  10.1152/ajplung.00221.2011
[31] DEUSE T, HUA X, WANG D, et al. Dichloroacetate prevents restenosis in preclinical animal models of vessel injury[J]. Nature,2014,509(7502):641-644. doi:  10.1038/nature13232
[32] VALBUENA G N, RIZZARDINI M, CIMINI S, et al. Metabolomic analysis reveals increased aerobic glycolysis and amino acid deficit in a cellular model of amyotrophic lateral sclerosis[J]. Mol Neurobiol,2016,53(4):2222-2240. doi:  10.1007/s12035-015-9165-7
[33] PALAMIUC L, SCHLAGOWSKI A, NGO S T, et al. A metabolic switch toward lipid use in glycolytic muscle is an early pathologic event in a mouse model of amyotrophic lateral sclerosis[J]. EMBO Mol Med,2015,7(5):526-546. doi:  10.15252/emmm.201404433
[34] MIQUEL E, CASSINA A, MARTÍNEZ-PALMA L, et al. Modulation of astrocytic mitochondrial function by dichloroacetate improves survival and motor performance in inherited amyotrophic lateral sclerosis[J]. PLoS One,2012,7(4):e34776. doi:  10.1371/journal.pone.0034776
[35] JOHNSTONE T C, KULAK N, PRIDGEN E M, et al. Nanoparticle encapsulation of mitaplatin and the effect thereof on in vivo properties[J]. ACS Nano,2013,7(7):5675-5683. doi:  10.1021/nn401905g
[36] SAHA S, GHOSH M, DUTTA S K. A potent tumoricidal co-drug “Bet-CA”: an ester derivative of betulinic acid and dichloroacetate selectively and synergistically kills cancer cells[J]. Sci Rep,2015,5:7762. doi:  10.1038/srep07762
[37] FULDA S, KROEMER G. Targeting mitochondrial apoptosis by betulinic acid in human cancers[J]. Drug Discov Today,2009,14(17-18):885-890. doi:  10.1016/j.drudis.2009.05.015
[38] PATHAK R K, MARRACHE S, HARN D A, et al. Mito-DCA: a mitochondria targeted molecular scaffold for efficacious delivery of metabolic modulator dichloroacetate[J]. ACS Chem Biol,2014,9(5):1178-1187. doi:  10.1021/cb400944y
[39] TRAPELLA C, VOLTAN R, MELLONI E, et al. Design, synthesis, and biological characterization of novel mitochondria targeted dichloroacetate-loaded compounds with antileukemic activity[J]. J Med Chem,2016,59(1):147-156. doi:  10.1021/acs.jmedchem.5b01165
[40] ZHANG S L, HU X, ZHANG W, et al. Unexpected discovery of dichloroacetate derived adenosine triphosphate competitors targeting pyruvate dehydrogenase kinase to inhibit cancer proliferation[J]. J Med Chem,2016,59(7):3562-3568. doi:  10.1021/acs.jmedchem.5b01828
[41] (NTP) N T P. NTP technical report on the toxicology studies of bromodichloroacetic acid (CASRN 7133-14-7) in F344/N rats and B6C3F1/N mice and toxicology and carcinogenesis studies of bromodichloroacetic acid in F344/NTac rats and B6C3F1/N mice (drinking water studies)[R]. NIEHS, 2015.
[42] IARC Working Group on the Evaluation of Carcinogenic Risks to Humans. Some drinking-water disinfectants and contaminants, including arsenic. Monographs on chloramine, chloral and chloral hydrate, dichloroacetic acid, trichloroacetic acid and 3-chloro-4-(dichloromethyl)-5-hydroxy-2(5H)-furanone[S]. IARC Monogr Eval Carcinog Risks Hum, 2004, 84: 269-477.
[43] STACPOOLE P W, HENDERSON G N, YAN Z M, et al. Pharmacokinetics, metabolism, and toxicology of dichloroacetate[J]. Drug Metab Rev,1998,30(3):499-539. doi:  10.3109/03602539808996323
[44] DEANGELO A B, GEORGE M H, HOUSE D E. Hepatocarcinogenicity in the male B6C3F1 mouse following a lifetime exposure to dichloroacetic acid in the drinking water: dose-response determination and modes of action[J]. J Toxicol Environ Health A,1999,58(8):485-507. doi:  10.1080/009841099157115
[45] BULL R J, ORNER G A, CHENG R S, et al. Contribution of dichloroacetate and trichloroacetate to liver tumor induction in mice by trichloroethylene[J]. Toxicol Appl Pharmacol,2002,182(1):55-65. doi:  10.1006/taap.2002.9427
[46] STACPOOLE P W. Controlled clinical trial of dichloroacetate for treatment of congenital lactic acidosis in children[J]. PEDIATRICS,2006,117(5):1519-1531. doi:  10.1542/peds.2005-1226
[47] STACPOOLE P W, HARWOOD H J Jr, CAMERON D F Jr, et al. Chronic toxicity of dichloroacetate: Possible relation to thiamine deficiency in rats[J]. Fundam Appl Toxicol,1990,14(2):327-337. doi:  10.1016/0272-0590(90)90212-3
[48] STACPOOLE P W, HENDERSON G N, YAN Z, et al. Clinical pharmacology and toxicology of dichloroacetate[J]. Environ Health Perspect,1998,106(Suppl 4):989-994. doi:  10.1289/ehp.98106s4989