Protein Information

Name lactate dehydrogenase (protein family or complex)
Synonyms LDH; lactate dehydrogenase; lactate dehydrogenases

Compound Information

Name oxamate
CAS hexyl 2-(diethylamino)-2-oxoacetate

Reference List

PubMed Abstract RScore(About this table)
18577696 Lam CK, Chari M, Wang PY, Lam TK: Central lactate metabolism regulates food intake. Am J Physiol Endocrinol Metab. 2008 Aug;295(2):E491-6. Epub 2008 Jun 24.

Inhibition of central lactate metabolism to pyruvate with the lactate dehydrogenase inhibitor oxamate abolished the central effects of lactate on FI and BW.
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3768146 Strasser de Saad AM, Pesce de Ruiz Holgado AA, Oliver G: D-(+)-lactate dehydrogenase from Lactobacillus murinus. Biotechnol Appl Biochem. 1986 Oct;8(5):370-4.

Pyruvate analogs such as oxalate, oxamate, 2-oxobutyrate, and malonate acted as a competitive inhibitors.
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304854 Markwell JP, Lascelles J: Membrane-bound, pyridine nucleotide-independent L-lactate dehydrogenase of Rhodopseudomonas sphaeroides. J Bacteriol. 1978 Feb;133(2):593-600.

The enzyme activity was inhibited competitively by D-lactate and non-competitively by oxalate and oxamate.
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1731077 Wigley DB, Gamblin SJ, Turkenburg JP, Dodson EJ, Piontek K, Muirhead H, Holbrook JJ: Structure of a ternary complex of an allosteric lactate dehydrogenase from Bacillus stearothermophilus at 2.5 A resolution. J Mol Biol. 1992 Jan 5;223(1):317-35.

Interactions between the protein and bound coenzyme and oxamate are described in relation to other studies using site-specific mutagenesis.
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168830 Sanchez JJ, Palleroni NJ, Doudoroff M: Lactate dehydrogenases in cyanobacteria. Arch Microbiol. 1975 Jun 20;104(1):57-65.

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3430126 Holt RW, Leibel WS: Coexpression of distinct eye- and liver-specific LDH isozymes in cichlid fish. J Exp Zool. 1987 Nov;244(2):337-43.

In a recent electrophoretic survey of lactate dehydrogenase (LDH) in neotropical cichlid fishes (Perciformes, Cichlidae) we have discovered several species in which a cathodal liver-specific isozyme is expressed along with the highly-anodal eye-specific isozyme (LDH-C4) typically encountered in perciform fishes.
Preliminary characterization of the liver-specific isozyme relative to the eye-specific LDH-C4 in the Basketmouth cichlid with respect to thermolability and NADH-induced binding to oxamate-sepharose columns suggests that the eye- and liver-specific LDH isozymes are biochemically quite distinct in this fish and that they are probably encoded by two distinct loci.
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7358131 Toowicharanont P, Svasti J: A logical approach to the isolation of lactate dehydrogenase isozyme X from human testes: a general rationale for the isolation of homotetrameric LDH isozymes. Experientia. 1980 Jan 15;36(1):37-8.

Immunoadsorbent and oxamate-Sepharose chromatography were used to isolate electrophoretically homogeneous LDH-X from human testes with a final specific activity of 125 IU/mg and good yields: other applications of this appraoch are discussed.
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1989512 Chang GG, Huang SM, Chiou SH: Kinetic mechanism of the endogenous lactate dehydrogenase activity of duck epsilon-crystallin. Arch Biochem Biophys. 1991 Feb 1;284(2):285-91.

D-Lactate, tartronate, and oxamate were strong dead-end inhibitors for the lactate dehydrogenase activity of epsilon-crystallin.
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9446610 Fushinobu S, Ohta T, Matsuzawa H: Homotropic activation via the subunit interaction and allosteric symmetry revealed on analysis of hybrid enzymes of L-lactate dehydrogenase. J Biol Chem. 1998 Jan 30;273(5):2971-6.

Oxamate, a competitive inhibitor of L-lactate dehydrogenase, was used to mimic the substrate-induced activation of the wild-type subunit as "a regulatory subunit." The malate dehydrogenase activity of the mutant subunit as "the catalytic subunit" of the hybrid enzymes was measured, and the activity of the mutant subunit was activated on the addition of oxamate.
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18710947 Milovanova TN, Bhopale VM, Sorokina EM, Moore JS, Hunt TK, Hauer-Jensen M, Velazquez OC, Thom SR: Lactate stimulates vasculogenic stem cells via the thioredoxin system and engages an autocrine activation loop involving hypoxia-inducible factor 1. Mol Cell Biol. 2008 Oct;28(20):6248-61. Epub 2008 Aug 18.

SPC recruitment and protein changes were inhibited by siRNA specific to lactate dehydrogenase, TrxR, or HIF-1 and by oxamate, apocynin, U0126, N-acetylcysteine, dithioerythritol, and antibodies to VEGF or SDF-1.
31(0,1,1,1) Details
7779436 Hamilton E, Fennell M, Stafford DM: Modification of tumour glucose metabolism for therapeutic benefit. Acta Oncol. 1995;34(3):429-33.

Cellular ATP fell during exposure of cells in air to 2-deoxy glucose or to the lactate dehydrogenase inhibitor oxamate.
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16308838 Meissner T, Friedmann B, Okun JG, Schwab MA, Otonkoski T, Bauer T, Bartsch P, Mayatepek E: Massive insulin secretion in response to anaerobic exercise in exercise-induced hyperinsulinism. Horm Metab Res. 2005 Nov;37(11):690-4.

The activity of lactate dehydrogenase of the index patient in isolated leukocytes as well as the response to inhibition of oxamate was normal.
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174737 Trommer WE, Becker G: The separation of partially modified lactate dehydrogenase by affinity chromatography. Biochim Biophys Acta. 1976 Jan 23;422(1):1-7.

The resulting protein mixture was separated by affinity chromatography on a Sepharose-linked oxamate column yielding three distinct enzyme fractions with one, two and three out of four subunits being modified.
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6628830 Yamamoto S: H4-isozyme of lactate dehydrogenase in a solution of sodium C chloride--6. Int J Biochem. 1983;15(10):1279-82.

The effect of oxalate and oxamate on the molecular weight..
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1036172 Gimeno AL, Goldraij A, Gimeno MF, Santillan de Torres R: Effects of oxamate, an inhibitor of lactate dahydrogenase, upon the spontaneous or oxytocin-induced motility and over pyruvate levels of uterine horns isolated from ovariectomized or estrus rats. Reproduccion. 1976 Jan-Jun;3(1-2):5-14.

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2160721 Mazo A, Forner A, Domenech C, Busquets M, Gelpi JL, Cortes A: Comparative analysis of the reduction of oxaloacetate by human hepatoma and normal liver extracts. Tumour Biol. 1990;11(3):120-8.

Experiments performed with mixtures of both purified enzymes and, conversely, by using oxamate, a specific inhibitor of lactate dehydrogenase, reveal that the deviation in Michaelis-Menten behavior observed is due to the oxaloacetate reductase activity of lactate dehydrogenase instead of the presence of a novel malate dehydrogenase isoenzyme.
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16665088 Hoffman NE, Hanson AD: Purification and Properties of Hypoxically Induced Lactate Dehydrogenase from Barley Roots. Plant Physiol. 1986 Nov;82(3):664-670.

Using Affigel Blue and oxamate-agarose affinity chromatography, lactate dehydrogenase (LDH) was purified 2000-fold from hypoxically induced barley roots.
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4359923 Bennett NG, Gutfreund H: The kinetics of the interconversion of intermediates of the reaction of pig muscle lactate dehydrogenase with oxidized nicotinamide-adenine dinucleotide and lactate. Biochem J. 1973 Sep;135(1):81-5.

Oxamate competes with pyruvate for the substrate binding site on the E (NADH) complex of pig skeletal muscle lactate dehydrogenase.
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9428654 Wong C, Rodriguez-Paez L, Nogueda B, Perez A, Baeza I: Selective inhibition of the sperm-specific lactate dehydrogenase isozyme-C4 by N-isopropyl oxamate. Biochim Biophys Acta. 1997 Nov 14;1343(1):16-22.
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11007175 Mulkiewicz E, Zietara MS, Stachowiak K, Skorkowski EF: Properties of lactate dehydrogenase from the isopod, Saduria entomon. Comp Biochem Physiol B Biochem Mol Biol. 2000 Jul;126(3):337-46.

Saduria entomon lactate dehydrogenase (LDH-A4*) from thorax muscle was purified about 89 fold to specific activity 510 micromol NADH/min/mg using Cibacron Blue 3GA Agarose and Oxamate-Agarose chromatographies.
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94928 Henkel E: [Kinetic determination of alpha-amylase in serum and urine with an oligosaccharide as substrate--modification for a fully mechanized enzyme measuring device (author's transl)]. J Clin Chem Clin Biochem. 1979 Nov;17(11):705-8.

Thereafter the lactate dehydrogenase reaction is stopped by addition of oxamate and the alpha-amylase activity is measured.
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36072 Bloxham DP, Sharma RP, Wilton DC: A detailed investigation of the properties of lactate dehydrogenase in which the 'Essential' cysteine-165 is modified by thioalkylation. Biochem J. 1979 Mar 1;177(3):769-80.

However, the affinity of oxamate for the enzyme--NADH complex was decreased by 100-fold and it was calculated that this constituted a net increase of 10.4 kJ/mol in the activation energy for binding.
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17636950 Choi SR, Pradhan A, Hammond NL, Chittiboyina AG, Tekwani BL, Avery MA: Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors. J Med Chem. 2007 Aug 9;50(16):3841-50. Epub 2007 Jul 18.

It is known that the oxamate moiety, a pyruvate analog, alone shows higher inhibition against pfLDH than human LDHs, suggesting that it can be used for the development of selective inhibitors.
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1996957 LeVan KM, Goldberg E: Properties of human testis-specific lactate dehydrogenase expressed from Escherichia coli. Biochem J. 1991 Feb 1;273 ( Pt 3):587-92.

Human LDH-C4 was purified over 200-fold from litre cultures of cells by AMP and oxamate affinity chromatography to a specific activity of 106 units/mg.
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9655830 Auerbach G, Ostendorp R, Prade L, Korndorfer I, Dams T, Huber R, Jaenicke R: Lactate dehydrogenase from the hyperthermophilic bacterium thermotoga maritima: the crystal structure at 2.1 A resolution reveals strategies for intrinsic protein stabilization. Structure. 1998 Jun 15;6(6):769-81.

RESULTS: The crystal structure of the extremely thermostable TmLDH has been determined at 2.1 A resolution as a quaternary complex with the cofactor NADH, the allosteric activator fructose-1,6-bisphosphate, and the substrate analog oxamate.
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9041714 Sugiyama N, Taniguchi N: Evaluation of the role of lactate dehydrogenase in oxalate synthesis. . Phytochemistry. 1997 Feb;44(4):571-4.

LDH was purified by affinity chromatography on affigel blue and oxamate agarose columns.
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15980172 McClendon S, Zhadin N, Callender R: The approach to the Michaelis complex in lactate dehydrogenase: the substrate binding pathway. Biophys J. 2005 Sep;89(3):2024-32. Epub 2005 Jun 24.

We examine here the dynamics of forming the Michaelis complex of the enzyme lactate dehydrogenase by characterizing the binding kinetics and thermodynamics of oxamate (a substrate mimic) to the binary lactate dehydrogenase/NADH complex over multiple timescales, from nanoseconds to tens of milliseconds.
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11415458 Cortes A, Cascante M, Cardenas ML, Cornish-Bowden A: Relationships between inhibition constants, inhibitor concentrations for 50% inhibition and types of inhibition: new ways of analysing data. Biochem J. 2001 Jul 1;357(Pt 1):263-8.

The type of analysis proposed has been tested experimentally by examining inhibition of lactate dehydrogenase by oxalate (an uncompetitive inhibitor with respect to pyruvate) and oxamate (a competitive inhibitor with respect to pyruvate), and of cytosolic malate dehydrogenase by hydroxymalonate (a mixed inhibitor with respect to oxaloacetate).
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6357283 Asker H, Davies D: Purification of rat liver enzymes involved in the oxidation of glyoxylate. . Biochim Biophys Acta. 1983 Nov 22;761(1):103-8.

The use of Sepharose aminohexyl oxamate for the purification of glycolate oxidase and lactate dehydrogenase is described.
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7839663 Sevriukov EA, Evseev LP: [Isolation of lactate dehydrogenase-C4 from human spermatozoa] . Vopr Med Khim. 1994 Sep-Oct;40(5):23-5.

LDH C4 was isolated as follows: precipitation with ammonium sulfate, separation of LDH C4 from other LDH isoenzymes using immunosorbents, purification from contaminating proteins of oxamate-Sepharose.
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4650384 Wilkinson JH, Walter SJ: Oxamate as a differential inhibitor of lactate dehydrogenase isoenzymes. Enzyme. 1972;13(4):170-6.
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19023021 Milovanova TN, Bhopale VM, Sorokina EM, Moore JS, Hunt TK, Hauer-Jensen M, Velazquez OC, Thom SR: Hyperbaric oxygen stimulates vasculogenic stem cell growth and differentiation in vivo. J Appl Physiol. 2009 Feb;106(2):711-28. Epub 2008 Nov 20.

Cell recruitment to Matrigel and protein synthesis responses were abrogated by N-acetyl cysteine, dithioerythritol, oxamate, apocynin, U-0126, neutralizing anti-vascular endothelial growth factor, or anti-stromal cell-derived factor-1 antibodies, and small inhibitory RNA to Trx reductase, lactate dehydrogenase, gp91 (phox), HIF-1 or -2, and in mice conditionally null for HIF-1 in myeloid cells.
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4763379 McPherson A Jr: Binding of oxamate to the apoenzyme of dogfish M4 lactate dehydrogenase. J Mol Biol. 1973 Jun 5;76(4):528-31.
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7305938 Bloxham DP: The chemical reactivity of the histidine-195 residue in lactate dehydrogenase thiomethylated at the cysteine-165 residue. Biochem J. 1981 Jan 1;193(1):93-7.

This reaction was not affected in the enzyme-NADH binary complex, but was diminished in the enzyme-NADH-oxamate ternary complex.
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234418 Gordon GL, Doelle HW: Production of racemic lactic acid in Pediococcus cerevisiae cultures by two lactate dehydrogenases. J Bacteriol. 1975 Feb;121(2):600-7.

The enzymes obey Michaelis-Menten kinetics for both pyruvate and reduced NAD at pH 5.4 and 7.4, with increased affinity for both substrates at the acid pH. alpha-Ketobutyrate can be used as a reducible substrate, whereas oxamate has no inhibitory effect on lactate oxidation by either enzyme.
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6825698 Steinbuchel A, Schlegel HG: NAD-linked L (+)-lactate dehydrogenase from the strict aerobe alcaligenes eutrophus. 2. Eur J Biochem. 1983 Feb 1;130(2):329-34.

The enzyme is strongly inhibited by oxaloacetate, oxalate and to a less extent by oxamate.
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3192948 Decker T, Lohmann-Matthes ML: A quick and simple method for the quantitation of lactate dehydrogenase release in measurements of cellular cytotoxicity and tumor necrosis factor (TNF) activity. J Immunol Methods. 1988 Nov 25;115(1):61-9.

LDH activity was determined as NADH oxidation or INT reduction over a defined time interval, which was limited by stopping the enzymatic reaction with the inhibitor oxamate.
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3311154 De Weck Z, Pande J, Kagi JH: Interdependence of coenzyme-induced conformational work and binding potential in yeast alcohol and porcine heart lactate dehydrogenases: a hydrogen-deuterium exchange study. Biochemistry. 1987 Jul 28;26(15):4769-76.

Ternary complexes such as YADH-NAD+-pyrazole, PHLDH-NAD+-oxalate, and PHLDH-NADH-oxamate, which mimic the transition state, have a significantly more pronounced effect on exchange rates than the corresponding binary complexes.
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15875809 Pamp K, Bramey T, Kirsch M, De Groot H, Petrat F: NAD (H) enhances the Cu (II)-mediated inactivation of lactate dehydrogenase by increasing the accessibility of sulfhydryl groups. Free Radic Res. 2005 Jan;39(1):31-40.

LDH activity was preserved by thiol donators and pyruvate and partially preserved by lactate and oxamate.
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3010655 Mothersill C, Seymour CB: Effect of lactate on the recovery of CHO-KI cells from gamma radiation damage. Acta Radiol Oncol. 1986 Jan-Feb;25(1):71-6.

To investigate a possible involvement of NADH generation via lactate dehydrogenase in the mechanism, oxamate, a non-metabolisable analogue of lactate, was investigated.
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1264235 Hochachka PW, Norberg C, Baldwin J, Fields JH: Enthalpy-entropy compensation of oxamate binding by homologous lactate dehydrogenases. Nature. 1976 Apr 15;260(5552):648-50.
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17567242 Hunt TK, Aslam RS, Beckert S, Wagner S, Ghani QP, Hussain MZ, Roy S, Sen CK: Aerobically derived lactate stimulates revascularization and tissue repair via redox mechanisms. Antioxid Redox Signal. 2007 Aug;9(8):1115-24.

Furthermore, inhibition of lactate dehydrogenase by using oxamate also prevented the angiogenic effects of lactate.
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19523445 Cha SH, Lane MD: Central lactate metabolism suppresses food intake via the hypothalamic AMP kinase/malonyl-CoA signaling pathway. Biochem Biophys Res Commun. 2009 Aug 14;386(1):212-6. Epub 2009 Jun 10.

All downstream effects of hypothalamic lactate are blocked by icv administered oxamate, a potent inhibitor of lactate dehydrogenase, thus verifying the central action of lactate.
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4369310 Whitaker JR, Yates DW, Bennett NG, Holbrook JJ, Gutfreund H: The identification of intermediates in the reaction of pig heart lactate dehydrogenase with its substrates. Biochem J. 1974 Jun;139(3):677-97.

Several inhibitory complexes have also been studied including E (NAD+) (Oxamate) and E (NADH) (Oxamate') and the abortive ternary complex E (NADH) (Lactate).
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6499843 Taguchi H, Matsuzawa H, Ohta T: L-Lactate dehydrogenase from Thermus caldophilus GK24, an extremely thermophilic bacterium. Eur J Biochem. 1984 Dec 3;145(2):283-90.

Heat-stable and fructose-1,6-bisphosphate-activated L-lactate dehydrogenase (EC 1.1.1.27) has been purified from an extremely thermophilic bacterium, Thermus caldophilus GK24 [Taguchi, H., Yamashita, M., Matsuzawa, H. and Ohta, T. (1982) J.
On modification reaction with 2,3-butanedione in the presence of NADH and oxamate, an enhanced activity of the T. caldophilus L-lactate dehydrogenase was obtained independently of fructose 1,6-bisphosphate, and the modified enzyme was desensitized to fructose 1,6-bisphosphate.
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18253497 Lemire J, Mailloux RJ, Appanna VD: Mitochondrial lactate dehydrogenase is involved in oxidative-energy metabolism in human astrocytoma cells (CCF-STTG1). PLoS One. 2008 Feb 6;3(2):e1550.

Oxamate, an inhibitor of lactate dehydrogenase (LDH), abolished mitochondrial lactate consumption.
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2504292 Warth E, Jacobi T, Woenckhaus C: Preparation and properties of a holo-lactate dehydrogenase enzyme reactor. Biochimie. 1989 May;71(5):613-23.

Both enzymes were cross-linked by dimethyl suberimidate in the presence or absence of NAD+, bis-NAD+, pyruvate, and oxamate.
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535158 Lustig V, Redman LW: Improved serum initiated aspartate aminotransferase assay by inhibition of lactate dehydrogenase with oxamate. Clin Biochem. 1979 Dec;12(6):254-5.
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392504 Reider E, Wagner EF, Schweiger M: Control of phosphoenolpyruvate-dependent phosphotransferase-mediated sugar transport in Escherichia coli by energization of the cell membrane. Proc Natl Acad Sci U S A. 1979 Nov;76(11):5529-33.

Oxamate, a specific inhibitor of lactate dehydrogenase, prevented the inhibitory effect of D-lactate.
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4321894 Holbrook JJ, Stinson RA: Reactivity of the essential thiol group of lactate dehydrogenase and substrate binding. Biochem J. 1970 Nov;120(2):289-97.

The inhibited enzymes fail to bind C (2) and C (3) molecules to give the ternary complexes enzyme-NAD (+)-pyruvate, enzyme-NADH-oxamate and enzyme-NADH-oxalate.
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4019440 Machida M, Matsuzawa H, Ohta T: Fructose 1,6-bisphosphate-dependent L-lactate dehydrogenase from Thermus aquaticus YT-1, an extreme thermophile: activation by citrate and modification reagents and comparison with Thermus caldophilus GK24 L-lactate dehydrogenase. J Biochem. 1985 Mar;97(3):899-909.

The enzymes modified with 2,3-butanedione, acetic anhydride and diethyl pyrocarbonate in the presence of both NADH and oxamate were desensitized to fructose 1,6-bisphosphate, and the modified enzymes were active even in the absence of fructose 1,6-bisphosphate.
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16112812 O'Flaherty C, Breininger E, Beorlegui N, Beconi MT: Acrosome reaction in bovine spermatozoa: role of reactive oxygen species and lactate dehydrogenase C4. Biochim Biophys Acta. 2005 Oct 30;1726(1):96-101. Epub 2005 Aug 8.

Sodium oxamate, an inhibitor of LDH-C4, prevented the AR induced by lysophosphatidylcholine (LPC) or NADH.
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226147 Wenzel HR, Trommer WE: Ternary complex formation of pig heart lactate dehydrogenase with spin-labelled coenzyme and inhibitors as studied by electron spin resonance. Biochim Biophys Acta. 1979 Jun 6;568(2):287-96.

Dissociation constants calculated for the inhibitors oxamate and oxalate from their corresponding ternary complexes are in excellent agreement with data from literature derived from sedimentation experiments.
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11276087 Read JA, Winter VJ, Eszes CM, Sessions RB, Brady RL: Structural basis for altered activity of M- and H-isozyme forms of human lactate dehydrogenase. Proteins. 2001 May 1;43(2):175-85.

Both structures have been crystallized as ternary complexes in the presence of the NADH cofactor and oxamate, a substrate-like inhibitor.
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182202 Schmid F, Hinz HJ, Jaenicke R: Thermodynamic studies of binary and ternary complexes of pig heart lactate dehydrogenase. Biochemistry. 1976 Jul 13;15(14):3052-9.

The thermodynamics of the reaction catalyzed by pig heart muscle lactate dehydrogenase (LDH; EC1.1.1,27) have been studied in 0,2 M potassium phosphate buffer, pH 7, over the temperature range of 10 to 35 degrees C by using oxamate and oxalate to simulate the corresponding reactions of the substrates pyruvate and lactate, respectively.
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8309939 Carlsson H, Prachayasittikul V, Bulow L: Zinc ions bound to chimeric His4/lactate dehydrogenase facilitate decarboxylation of oxaloacetate. Protein Eng. 1993 Nov;6(8):907-11.

The gene product, His4/lactate dehydrogenase, could be purified to homogeneity using either immobilized metal (Zn2+)-affinity chromatography or affinity chromatography on oxamate agarose.
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114469 Schar HP, Zuber H: Structure and function of L-lactate dehydrogenases from thermophilic and mesophilic bacteria. Hoppe Seylers Z Physiol Chem. 1979 Jul;360(7):795-807.

The tetrameric enzymes were characterized with respect to thermostability, pH and temperature dependence of the pyruvate reduction and the L-lactate oxidation, substrate specificity, saturation kinetics (Km values of pyruvate, lactate, NAD, NADH), pyruvate and oxamate inhibition, and activation by fructose bisphosphate.
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170258 Chan PC, Bielski BH: Lactate dehydrogenase-catalyzed stereospecific hydrogen atom transfer from reduced nicotinamide adenine dinucleotide to dicarboxylate radicals. J Biol Chem. 1975 Sep 25;250(18):7266-71.

The hydrogen atom transfer was inhibited by oxamate.
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6402502 Mueller PR, Collins ML: Identification of two distinct lactate dehydrogenases in Rhodospirillum rubrum. J Bacteriol. 1983 Mar;153(3):1562-6.

Crossed immunoelectrophoretic analysis revealed two antigenically distinct enzymes that were further distinguished by specificity for d- and l-stereoisomers of lactate and by the sensitivity of the d-lactate dehydrogenase to inhibition by oxamate and oxalate.
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3065514 Wigley DB, Muirhead H, Gamblin SJ, Holbrook JJ: Crystallization of a ternary complex of lactate dehydrogenase from Bacillus stearothermophilus. J Mol Biol. 1988 Dec 20;204(4):1041-3.

All of these crystal forms were grown in the presence of NADH, sodium oxamate and fructose 1,6-bisphosphate.
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2330370 Piontek K, Chakrabarti P, Schar HP, Rossmann MG, Zuber H: Structure determination and refinement of Bacillus stearothermophilus lactate dehydrogenase. Proteins. 1990;7(1):74-92.

The structure of the activated holo-enzyme showed far greater similarity to the ternary complex of dogfish M4 lactate dehydrogenase with nicotinamide adenine dinucleotide and oxamate than to apo-M4 dogfish lactate dehydrogenase.
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3924858 Paoli C, Bardelli F, Rinaldi F, Donnini F, Tarli P: Biochemical purification of monkey and human LDH isoenzyme 5 suitable as immunization antigen. Ital J Biochem. 1985 Jan-Feb;34(1):11-8.

A method consisting in an ion-exchange chromatography on DEAE-Sephadex A50 and an affinity chromatography on Oxamate-hexyl-Sepharose for the purification of monkey and human LDH isoenzyme 5 is presented.
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6661190 Ward LD, Winzor DJ: Thermodynamic studies of the activation of rabbit muscle lactate dehydrogenase by phosphate. Biochem J. 1983 Dec 1;215(3):685-91.

Competitive-inhibition studies and fluorescence-quenching measurements indicated the lack of a phosphate effect on ternary-complex formation between enzyme-NADH complex and oxamate, a substrate analogue of pyruvate.
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7584602 Zietara MS, Skorkowski EF: Thermostability of lactate dehydrogenase LDH-A4 isoenzyme: effect of heat shock protein DnaK on the enzyme activity. Int J Biochem Cell Biol. 1995 Nov;27(11):1169-74.

The LDH-A4 isoenzyme was purified from fish skeletal muscle using the affinity chromatography on Oxamate-agarose.
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179609 Vorontsov EA, Lifshits NL, Mal'tsev NI, Iakovlev VA: [The interaction of pyridine-adenine-dinucleotides containing a hydrazide group with swine muscle lactate dehydrogenase]. Biokhimiia. 1976 Feb;41(2):248-54.

The comparison of the inhibitory ability of oxamate, incotinic acid hydraxide and their spin-labelled derivatives indicates the restricted and stiff sizes of a substrate-binding site.
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12075544 Collins ND, LeRoy BE, Vap L: Artifactually increased serum bicarbonate values in two horses and a calf with severe rhabdomyolysis. Vet Clin Pathol. 1998;27(3):85-90.

It was hypothesized that increased serum lactate dehydrogenase (LDH) activity and pyruvate concentration overwhelmed the oxamate LDH inhibitor in the enzymatic HCO3- assay, resulting in consumption of NADH and falsely elevated spectrophotometric reading.
It was hypothesized that increased serum lactate dehydrogenase (LDH) activity and pyruvate concentration overwhelmed the oxamate LDH inhibitor in the enzymatic HCO3- assay, resulting in consumption of NADH and falsely elevated spectrophotometric reading.
1(0,0,0,1) Details
2379665 Szczesna-Kaczmarek A: L-lactate oxidation by skeletal muscle mitochondria. . Int J Biochem. 1990;22(6):617-20.

Mitochondria isolated from rat skeletal muscle possess lactate dehydrogenase which is involved in direct oxidation of L-lactate in the presence of external NAD. 2.
Mitochondrial lactate oxidation is sensitive to oxamate-inhibitor of LDH, alpha-cyano-3-hydroxy-cinnamate-pyruvate translocase inhibitor and respiratory chain inhibitors (rotenone, antimycin A, KCN). 4.
1(0,0,0,1) Details
15552 Bloxham DP, Wilton DC: Modification of pig heart lactate dehydrogenase with methyl methanethiosulphonate to produce an enzyme with altered catalytic activity. Biochem J. 1977 Mar 1;161(3):643-51.

The modification of lactate dehydrogenase by methyl methanethiosulphonate involved the active site, since inhibition was completely prevented by substrate-analogue pairs such as NADH and oxamate or NAD+ and oxalate.
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2323817 Hillman JD, Duncan MJ, Stashenko KP: Cloning and expression of the gene encoding the fructose-1,6-diphosphate-dependent L-(+)-lactate dehydrogenase of Streptococcus mutans. Infect Immun. 1990 May;58(5):1290-5.

Of 18 reactive clones, 1 was found that expressed lactate dehydrogenase (LDH) activity identical to that of S. mutans with regard to dependence on fructose-1,6-diphosphate, thermal inactivation profile, and inhibition by sodium oxamate.
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3365414 Clarke AR, Wilks HM, Barstow DA, Atkinson T, Chia WN, Holbrook JJ: An investigation of the contribution made by the carboxylate group of an active site histidine-aspartate couple to binding and catalysis in lactate dehydrogenase. Biochemistry. 1988 Mar 8;27(5):1617-22.

Both bind pyruvate and its analogue (oxamate) 200 times more weakly than the wild-type enzyme but show little disruption in their binding of lactate and its unreactive analogue, trifluorolactate.
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9927705 Brooks GA, Dubouchaud H, Brown M, Sicurello JP, Butz CE: Role of mitochondrial lactate dehydrogenase and lactate oxidation in the intracellular lactate shuttle. Proc Natl Acad Sci U S A. 1999 Feb 2;96(3):1129-34.

As well, alpha-cyano-4-hydroxycinnamate (CINN), a known monocarboxylate transport inhibitor, and oxamate, a known LDH inhibitor were used.
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8532681 Philippopoulos M, Xiang Y, Lim C: Identifying the mechanism of protein loop closure: a molecular dynamics simulation of the Bacillus stearothermophilus LDH loop in solution. Protein Eng. 1995 Jun;8(6):565-73.

The 'loop' involving residues 98-110 in Bacillus stearothermophilus lactate dehydrogenase (BSLDH) is of great interest as substrate-induced 'loop' closure is thought to be rate-limiting and essential in catalyzing the reaction and in determining substrate specificity.
Consequently, we have explored the mechanism underlying 'loop' opening in BSLDH through a molecular dynamics simulation at high temperature (1000 K) in the presence of explicit solvent, starting from the X-ray structure of BSLDH complexed with the co-enzyme NAD+ and oxamate at 2.5 A.
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18922152 Thornburg JM, Nelson KK, Clem BF, Lane AN, Arumugam S, Simmons A, Eaton JW, Telang S, Chesney J: Targeting aspartate aminotransferase in breast cancer. . Breast Cancer Res. 2008;10(5):R84. Epub 2008 Oct 15.

Lactate dehydrogenase (LDH) regulates glycolytic flux by converting pyruvate to lactate and has been found to be highly expressed in breast tumours.
Oxamate is an inhibitor of both LDH and AAT, and we hypothesised that oxamate may disrupt the metabolism and growth of breast adenocarcinoma cells.
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12158558 Uchijima Y, Yoshida K, Saito H: [Effects of gossypol on human specific lactate dehydrogenase-C4 (LDH-C4)] Nippon Funin Gakkai Zasshi. 1989 Jan;34(1):165-8.

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17560727 Schurr A, Payne RS: Lactate, not pyruvate, is neuronal aerobic glycolysis end product: an in vitro electrophysiological study. Neuroscience. 2007 Jul 13;147(3):613-9. Epub 2007 Jun 8.

Here we employed electrophysiology of the rat hippocampal slice preparation to test and monitor the effects of malonate and oxamate, two different LDH inhibitors, and glutamate, a neuronal activator, in experiments, the results of which support the hypothesis that lactate, at least in this in vitro setting, is indeed the principal end product of neuronal aerobic glycolysis.
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2806266 Bergman DA, Winzor DJ: Thermodynamic nonideality in enzyme catalysis. Eur J Biochem. 1989 Oct 20;185(1):91-7.

As part of the search for a mechanistic explanation of this kinetic phenomenon, the space-filling effects of albumin have been used to eliminate the possibility that the increase in sedimentation coefficient of lactate dehydrogenase effected by inclusion of oxamate with enzyme-NADH complex reflects preferential binding of this pyruvate analog to a more compact isomeric state of the binary complex.
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8897500 Marchat L, Loiseau PM, Petek F: Purification and characterization of lactate dehydrogenase isoenzymes 1 and 2 from Molinema dessetae (Nematoda:Filarioidea). Parasitol Res. 1996;82(8):672-80.

Oxalate acted as a noncompetitive inhibitor of pyruvate reduction (Ki = 4.7 +/- 0.35 mM; mean +/- SEM, n = 10) and as a competitive inhibitor with lactate (Ki = 2.3 +/- 0.21 mM), whereas oxamate acted as a competitive inhibitor with pyruvate (Ki = 3.3 +/- 0.28 mM) and was noncompetitive with lactate (Ki = 19 +/- 1.2 mM).
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3606622 Hart KW, Clarke AR, Wigley DB, Chia WN, Barstow DA, Atkinson T, Holbrook JJ: The importance of arginine 171 in substrate binding by Bacillus stearothermophilus lactate dehydrogenase. Biochem Biophys Res Commun. 1987 Jul 15;146(1):346-53.

Replacement of this arginine by lysine has no effect on co-enzyme binding, a relatively small effect on the rate of turnover of the enzyme, but causes a 2000-fold increase in the Michaelis constant for pyruvate, a 6000-fold increase in the dissociation constant for oxamate and results in a Michaelis constant for lactate which is too high to measure.
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19429039 Bergold PJ, Pinkhasova V, Syed M, Kao HY, Jozwicka A, Zhao N, Coplan JD, Dow-Edwards D, Fenton AA: Production of panic-like symptoms by lactate is associated with increased neural firing and oxidation of brain redox in the rat hippocampus. Neurosci Lett. 2009 Apr 10;453(3):219-24. Epub 2009 Feb 23.

Lactate oxidized hippocampal redox since intrahippocampal injection of the LDH inhibitor, oxamate (50mM) prevented the oxidation of NADH/NAD (+) by IP lactate.
To enter intermediate metabolism, lactate is oxidized by lactate dehydrogenase (LDH) to pyruvate with co-reduction of NAD (+) to NADH.
1(0,0,0,1) Details
15909687 Larsen T: Determination of lactate dehydrogenase (LDH) activity in milk by a fluorometric assay. J Dairy Res. 2005 May;72(2):209-16.

Known inhibitors of LDH activity (oxidative direction), i.e., oxalic acid, oxamate, and pyruvate, were tested in different concentrations in order to verify the specificity of the response.
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8114106 Iwata S, Yoshida S, Ohta T: A regular 1:1 complex of two allosteric states in the single crystal of L-lactate dehydrogenase from Bifidobacterium longum. J Mol Biol. 1994 Feb 25;236(3):958-9.

Single crystals of the regular 1:1 complex of T and R-state tetramers of L-lactate dehydrogenase from Bifidobacterium longum have been grown from polyethylene glycol 6000 solution in the presence of NADH, fructose 1,6-bisphosphate and oxamate.
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17316052 Choi SR, Beeler AB, Pradhan A, Watkins EB, Rimoldi JM, Tekwani B, Avery MA: Generation of oxamic acid libraries: antimalarials and inhibitors of Plasmodium falciparum lactate dehydrogenase. J Comb Chem. 2007 Mar-Apr;9(2):292-300. Epub 2007 Feb 23.

Oxamate, a competitive inhibitor, shows high substrate affinity for pfLDH.
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4336691 Brown AT, Wittenberger CL: Fructose-1,6-diphosphate-dependent lactate dehydrogenase from a cariogenic streptococcus: purification and regulatory properties. J Bacteriol. 1972 May;110(2):604-15.

The other pyruvate analogue, oxamate, inhibited enzyme activity at all pyruvate concentrations but had no effect on the sigmoidal nature of the pyruvate saturation curve or on the apparent kinetic order of the reaction with respect to substrate.
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5464273 Bacchi CJ, Ciaccio EI, O'Connell KM, Hutner SH: Biochemical properties of trypanosomatid lactate dehydrogenases. . J Bacteriol. 1970 Jun;102(3):826-34.

Comparison of trypanosomatid and human serum LDH enzymes with respect to K (m), substrate activity and inhibition, pH optima, and K (i) values for oxalate and oxamate indicated that the trypanosomatid isoenzymes differed significantly from serum LDH.
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17489101 Paventi G, Pizzuto R, Chieppa G, Passarella S: L-lactate metabolism in potato tuber mitochondria. . FEBS J. 2007 Mar;274(6):1459-69.

Immunologic analysis by western blot using goat polyclonal anti-lactate dehydrogenase showed the existence of a mitochondrial lactate dehydrogenase, the activity of which could be measured photometrically only in mitochondria solubilized with Triton X-100.
The addition of L-lactate to potato tuber mitochondria caused: (a) a minor reduction of intramitochondrial pyridine nucleotides, whose measured rate of change increased in the presence of the inhibitor of the alternative oxidase salicyl hydroxamic acid; (b) oxygen consumption not stimulated by ADP, but inhibited by salicyl hydroxamic acid; and (c) activation of the alternative oxidase as polarographically monitored in a manner prevented by oxamate, an L-lactate dehydrogenase inhibitor.
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212270 Calvin J, Tubbs PK: Mitochondrial transport processes and oxidation of NADH by hypotonically-treated boar spermatozoa. Eur J Biochem. 1978 Aug 15;89(1):315-20.

Lactate-dependent NADH oxidation is inhibited by oxamate, an inhibitor of lactate dehydrogenase.
Lactate-dependent NADH oxidation is inhibited by oxamate, an inhibitor of lactate dehydrogenase.
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466765 Rej R: Measurement of aspartate aminotransferase activity: effects of oxamate. . Clin Chem. 1979 Apr;25(4):555-9.

Oxamate, a potent inhibitor of lactate dehydrogenase, is shown also to inhibit aspartate aminotransferase activity, both in human serum and in purified isoenzymes of human origin.
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213050 Kolk AH, van Kuyk L, Boettcher B: Isolation of human lactate dehydrogenase isoenzyme X by affinity chromatography. Biochem J. 1978 Sep 1;173(3):767-71.

Human isoenzyme LDH-X (lactate dehydrogenase isoenzyme X) was isolated from seminal fluid of frozen semen samples by affinity chromatography by using oxamate-Sepharose and AMP-Sepharose.
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17483169 Qiu L, Gulotta M, Callender R: Lactate dehydrogenase undergoes a substantial structural change to bind its substrate. Biophys J. 2007 Sep 1;93(5):1677-86. Epub 2007 May 4.

The on-rate of the formation of the encounter complex from LDH/NADH with oxamate (a substrate mimic) is determined as a function of temperature and in the presence of small concentrations of a protein destabilizer (urea) and protein stabilizer (TMAO).
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11966575 O'Flaherty CM, Beorlegui NB, Beconi MT: Lactate dehydrogenase-C4 is involved in heparin- and NADH-dependent bovine sperm capacitation. Andrologia. 2002 Apr;34(2):91-7.

LDH-C4 activity was 5.52 +/- 3.41, 15.72 +/- 6.04 and 15.22 +/- 1.92 Units 1010 spermatozoa-1 in plasma membrane, sperm suspension and cytosol fraction, respectively; these activities were inhibited by sodium oxamate.
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175780 Chen SS, Engel PC: Dogfish M4 lactate dehydrogenase: reversible inactivation by pyridoxal 5'-phosphate and complete protection in complexes that mimic the active ternary complex. Biochem J. 1975 Nov;151(2):447-9.

The activity is completely protected in the complexes E-NAD+-oxalate, E-NADH-oxamate and E-(NAD+-pyruvate adduct), but only partially protected in E-NAD+, E-NADH, E-NAD+-oxamate and E-NADH-oxalate.
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242300 Gotz F, Schleifer KH: Purification and properties of a fructose-1,6-diphosphate activated L-lactate dehydrogenase from Staphylococcus epidermidis. Arch Microbiol. 1975 Nov 7;105(3):303-12.

The enzyme activity was inhibited by adenosine diphosphate (ADP) and oxamate.
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3769523 Rohde MD, Huff JW: Contact lens-induced edema in vitro--amelioration by lactate dehydrogenase inhibitors. Curr Eye Res. 1986 Oct;5(10):751-8.

The pronounced swelling induced by PMMA lens placement was much less however, in the epithelial presence of 3.2 mM sodium oxalate (3.22 microns/hr) or 3.2 mM sodium oxamate (5.38 microns/hr).
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3271903 Sasaki Y, Sato N, Yamada S: [Properties of dental pulp lactate dehydrogenase. Meikai Daigaku Shigaku Zasshi. 1988;17(1):66-79.

Effects of oxamate and oxalate]
1(0,0,0,1) Details
19683593 Si Y, Shi H, Lee K: Impact of perturbed pyruvate metabolism on adipocyte triglyceride accumulation. Metab Eng. 2009 Nov;11(6):382-90. Epub 2009 Aug 14.


We treated cultured 3T3-L1 adipocytes with chemical inhibitors of lactate dehydrogenase (LDH) and pyruvate carboxylase (PC), and characterized their global effects on intermediary metabolism using metabolic flux and isotopomer analysis.
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6819859 Onoufriou A, Alahiotis SN: Drosophila lactate dehydrogenase: molecular and genetic aspects. Biochem Genet. 1982 Dec;20(11-12):1195-1209.

(LDH) obtained from larvae of Drosophila melanogaster was purified to homogeneity by affinity chromatography on oxamate-Sepharose.
1(0,0,0,1) Details
7835319 Gawlita E, Anderson VE, Paneth P: Semiempirical calculations of the oxygen equilibrium isotope effect on binding of oxamate to lactate dehydrogenase. Eur Biophys J. 1994;23(5):353-60.
162(2,2,2,2) Details
7742308 Gawlita E, Paneth P, Anderson VE: Equilibrium isotope effect on ternary complex formation of [1-18O] oxamate with NADH and lactate dehydrogenase. Biochemistry. 1995 May 9;34(18):6050-8.
162(2,2,2,2) Details
7379304 Lustig V, Redman LW: Improved serum-initiated aspartate aminotransferase assay by inhibition of lactate dehydrogenase with oxamate. Clin Chem. 1980 Jun;26(7):831-4.
113(1,2,2,3) Details
666726 Kelly N, Delaney M, O'Carra P: Affinity chromatography of bacterial lactate dehydrogenases. . Biochem J. 1978 Jun 1;171(3):543-7.

The affinity system used was the immobilized oxamate derivative previously used to purify mammalian lactate dehydrogenases.
113(1,2,2,3) Details
11368947 Cassady CJ, Phillis JW, O'Regan MH: Further studies on the effects of topical lactate on amino acid efflux from the ischemic rat cortex. Brain Res. 2001 May 18;901(1-2):30-7.

The oxamate data indicate that inhibition of lactate dehydrogenase is detrimental to the viability of cortical cells during I/R, even though extracellular lactate levels are elevated.
112(1,2,2,2) Details
2735254 Uchijima Y, Yoshida K, Saito H: A further study of human seminal plasma lactate dehydrogenase-C4 (LDH-C4): kinetic properties of LDH-C4. Hinyokika Kiyo. 1989 Mar;35(3):457-63.

Lactate dehydrogenase-C4 (LDH-C4) from human seminal plasma was purified by 40-60% (NH4) 2SO4 precipitation, Oxamate-Sepharose 4B affinity column chromatography and AMP affinity column chromatography.
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3947644 Waldman AD, Birdsall B, Roberts GC, Holbrook JJ: 13C-NMR and transient kinetic studies on lactate dehydrogenase [Cys (13CN) 165]. Biochim Biophys Acta. 1986 Mar 7;870(1):102-11.

Formation of the ternary complexes E-NADH-oxamate and E-NAD+-oxalate results in an upfield shift of the signal of 1.2 ppm.
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9605319 Stoll VS, Manohar AV, Gillon W, MacFarlane EL, Hynes RC, Pai EF: A thioredoxin fusion protein of VanH, a D-lactate dehydrogenase from Enterococcus faecium: cloning, expression, purification, kinetic analysis, and crystallization. Protein Sci. 1998 May;7(5):1147-55.

Competitive inhibition constants for ADP-ribose, NAD+, and oxamate have also been determined.
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15051959 Duan C, Goldberg E: Inhibition of lactate dehydrogenase C4 (LDH-C4) blocks capacitation of mouse sperm in vitro. Cytogenet Genome Res. 2003;103(3-4):352-9.

Oxamate or its derivative was used to inhibit sperm LDH activity in a medium promoting capacitation.
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2691505 Iwata S, Minowa T, Mikami B, Morita Y, Ohta T: Crystallization of and preliminary crystallographic data for allosteric L-lactate dehydrogenase from Bifidobacterium longum. J Biochem. 1989 Oct;106(4):558-9.

Crystals grown in the presence of NADH (type II), both NADH and oxamate (type III), and NADH, oxamate, and FBP (type IV) were analyzed.
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2383305 Sarciron ME, Delabre-Defayolle I, Audin P, Petavy AF, Paris J: Effects of ethyl N-N-benzyl-methyl-oxamate in Meriones unguiculatus infected with Echinococcus multilocularis metacestodes. Arzneimittelforschung. 1990 May;40(5):607-10.

Ethyl N-N-benzyl-methyl-oxamate is a N-substituted derivative of the oxamic acid, well-known as inhibitor of the lactate dehydrogenase activity.
89(1,1,2,4) Details
182529 Spielmann H, Eibs HG, Mentzel C: Rapid purification of lactate dehydrogenase X from mouse testes by two steps of affinity chromatography on oxamate-sepharose. Experientia. 1976 Aug 15;32(8):1085-6.
87(1,1,2,2) Details
4352914 Holbrook JJ, Stinson RA: The use of ternary complexes to study ionizations and isomerizations during catalysis by lactate dehydrogenase. Biochem J. 1973 Apr;131(4):739-48.

The binding of oxamate to pig heart and pig muscle isoenzymes of lactate dehydrogenase in the presence of NADH was studied by fluorescence titration.
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7092806 Parker DM, Jeckel D, Holbrook JJ: Slow structural changes shown by the 3-nitrotyrosine-237 residue in pig heart [Tyr (3NO2) 237] lactate dehydrogenase. Biochem J. 1982 Mar 1;201(3):465-71.

The pKa of the phenolic hydroxy group of the Tyr (3NO2)-237 residue in pig heart [Tyr (3NO2) 237] lactate dehydrogenase is 7.2 in the apoenzyme, 7.4 in the enzyme-NADH complex and 7.8 in the enzyme-NADH-oxamate complex.
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20331438 Perez J, Hill BG, Benevides GA, Dranka BP, Darley-Usmar V: Role of cellular bioenergetics in smooth muscle cell proliferation induced by platelet-derived growth factor. Biochem J. 2010 Mar 24.

Moreover, L-lactate substitution for D-glucose was sufficient for increasing the mitochondrial reserve capacity and cell proliferation after treatment with PDGF; these effects were inhibited by the lactate dehydrogenase inhibitor, oxamate.
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11876643 Gulotta M, Deng H, Deng H, Dyer RB, Callender RH: Toward an understanding of the role of dynamics on enzymatic catalysis in lactate dehydrogenase. Biochemistry. 2002 Mar 12;41(10):3353-63.

The dynamics of the mobile loop, which closes over the active site and is important for catalysis and binding, were characterized by studies of the inhibitor oxamate binding to the LDH/NADH binary complex monitoring the changes in emission of bound NADH.
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18390601 Deng H, Brewer S, Vu DM, Clinch K, Callender R, Dyer RB: On the pathway of forming enzymatically productive ligand-protein complexes in lactate dehydrogenase. Biophys J. 2008 Jul;95(2):804-13. Epub 2008 Apr 4.

Isotope-edited static Fourier transform infrared studies on the bound oxamate protein complex reveal two kinds of oxamate environments: 1), a major populated structure wherein all significant hydrogen-bonding patterns are formed at the active site between protein and bound ligand necessary for the catalytically productive Michaelis complex and 2), a minor structure in a configuration of the active site that is unfavorable to carry out catalyzed chemistry.
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17396163 Fox JH, Kama JA, Lieberman G, Chopra R, Dorsey K, Chopra V, Volitakis I, Cherny RA, Bush AI, Hersch S: Mechanisms of copper ion mediated Huntington's disease progression. PLoS One. 2007 Mar 28;2(3):e334.

The LDH inhibitor oxamate resulted in neurodegeneration when delivered intra-striatially to healthy mice, indicating that LDH inhibition is relevant to neurodegeneration in HD.
We focused on two proteins: huntingtin, because of its centrality to HD, and lactate dehydrogenase (LDH), because of its documented sensitivity to copper, necessity for normoxic brain energy metabolism and evidence for altered lactate metabolism in HD brain.
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17556391 Yoshida Y, Holloway GP, Ljubicic V, Hatta H, Spriet LL, Hood DA, Bonen A: Negligible direct lactate oxidation in subsarcolemmal and intermyofibrillar mitochondria obtained from red and white rat skeletal muscle. J Physiol. 2007 Aug 1;582(Pt 3):1317-35. Epub 2007 Jun 7.

The lactate dehydrogenase (LDH) activity associated with SS and IMF mitochondria was 200- to 240-fold lower than in whole muscle.
Pyruvate and lactate oxidation were inhibited by alpha-cyano-4-hydroxycinnamate, while lactate oxidation was inhibited by oxamate.
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8548923 Chretien D, Pourrier M, Bourgeron T, Sene M, Rotig A, Munnich A, Rustin P: An improved spectrophotometric assay of pyruvate dehydrogenase in lactate dehydrogenase contaminated mitochondrial preparations from human skeletal muscle. Clin Chim Acta. 1995 Sep 15;240(2):129-36.

Using a model reaction system consisting of varying mixtures of purified lactate and pyruvate dehydrogenases, we found that the presence of oxamate, a competitive inhibitor of the lactate dehydrogenase, allowed the measurement of a linear rate of pyruvate dehydrogenase activity without interference from lactate dehydrogenase.
84(1,1,1,4) Details
175784 Brinkworth RI, Masters CJ, Winzor DJ: Evaluation of equilibrium constants for the interaction of lactate dehydrogenase isoenzymes with reduced nicotinamide-adenine dinucleotide by affinity chromatography. Biochem J. 1975 Dec;151(3):631-6.

Rabbit muscle lactate dehydrogenase was subjected to frontal affinity chromatography on Sepharose-oxamate in the presence of various concentrations of NADH and sodium phosphate buffer (0.05 M, pH 6.8) containing 0.5 M-NaCl.
83(1,1,1,3) Details
6934514 Tuengler P, Stein TN, Long GL: Studies on the active center of D- and L-lactate dehydrogenases using oxamate-diaminohexyl-Sepharose affinity chromatography. Proc Natl Acad Sci U S A. 1980 Oct;77(10):5832-6.
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19040414 Kokorovic A, Cheung GW, Rossetti L, Lam TK: Hypothalamic sensing of circulating lactate regulates glucose production. . J Cell Mol Med. 2008 Nov 14.

In the presence of physiologically-relevant increases in the levels of plasma lactate, inhibition of central lactate-sensing mechanisms by lactate dehydrogenase inhibitor oxamate or ATP-sensitive potassium channels blocker glibenclamide increased glucose production.
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8224107 Holmes LD, Schiller MR, Boeker EA: Kinetic analysis of lactate dehydrogenase using integrated rate equations. Experientia. 1993 Oct 15;49(10):893-901.

The inhibition constant for oxamate was also determined.
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3580377 Clarke AR, Wigley DB, Barstow DA, Chia WN, Atkinson T, Holbrook JJ: A single amino acid substitution deregulates a bacterial lactate dehydrogenase and stabilizes its tetrameric structure. Biochim Biophys Acta. 1987 May 27;913(1):72-80.

The mutation has not significantly changed the catalytic properties of the dimer (Kd NADH, Km pyruvate, Ki oxamate and kcat), but has weakened the binding of Fru-1,6-P2 to both the dimeric and tetrameric forms of the enzyme and has almost abolished any stimulatory effect.
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6640170 Torres-da Matta J, da Matta AN, Hasson-Voloch A: Electric organ lactate dehydrogenase:physical and kinetic properties of the purified enzyme from Electrophorus electricus (L.). Braz J Med Biol Res. 1983 Apr;16(1):1-10.

L (+) lactate dehydrogenase (LDH) from the electric organ of Electrophorus electricus (L.) was purified by ammonium sulfate precipitation, ion-exchange chromatography on DEAE-cellulose and gel filtration on Sephadex G-200.
Sodium oxamate behaved as a mixed inhibitor when lactate (NAD) was the substrate, whereas ethyl oxamate was an uncompetitive inhibitor.
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11396932 Jasso-Chavez R, Torres-Marquez ME, Moreno-Sanchez R: The Membrane-bound L- and D-lactate dehydrogenase activities in mitochondria from Euglena gracilis. Arch Biochem Biophys. 2001 Jun 15;390(2):295-303.

The activity of the pyridine nucleotide-independent lactate dehydrogenase (iLDH) was characterized in mitochondria isolated from the protist Euglena gracilis.
Oxamate was a competitive inhibitor against both L- and D-lactate.
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6384078 Wheeler PR, Bharadwaj VP, Katoch VM, Kannan KB: Lactate dehydrogenase in Mycobacterium leprae grown in armadillo liver. . Int J Lepr Other Mycobact Dis. 1984 Sep;52(3):371-6.

Since armadillo liver LDH isoenzymes with a similar electrophoretic mobility were shown to be considerably more sensitive to inhibition by oxamate than LDH in M. leprae extracts, it was confirmed that M. leprae grown in armadillo liver has its own LDH.
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1517347 Winzor DJ, Munro PD, Jackson CM: Study of high-affinity interactions by quantitative affinity chromatography. J Chromatogr. 1992 Apr 24;597(1-2):57-66.

Finally, published frontal affinity chromatographic data for the NADH-dependent elution of rabbit muscle lactate dehydrogenase from oxamate-Sepharose are reanalysed using these equations to demonstrate the characterization of a system reflecting the binding of a solute-ligand complex to an affinity matrix.
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