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Identification
NamePyruvic acid
Accession NumberDB00119  (NUTR00050)
TypeSmall Molecule
GroupsApproved, Nutraceutical
Description

An intermediate compound in the metabolism of carbohydrates, proteins, and fats. In thiamine deficiency, its oxidation is retarded and it accumulates in the tissues, especially in nervous structures. (From Stedman, 26th ed)

Structure
Thumb
Synonyms
2-ketopropionic acid
2-Oxopropanoic acid
2-Oxopropansaeure
2-Oxopropionsaeure
a-Ketopropionic acid
Acetylformic acid
Acide pyruvique
alpha-Ketopropionic acid
alpha-Oxopropionsaeure
Brenztraubensaeure
BTS
CH3COCOOH
Pyroracemic acid
Pyruvic acid
α-ketopropionic acid
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII8558G7RUTR
CAS number127-17-3
WeightAverage: 88.0621
Monoisotopic: 88.016043994
Chemical FormulaC3H4O3
InChI KeyInChIKey=LCTONWCANYUPML-UHFFFAOYSA-N
InChI
InChI=1S/C3H4O3/c1-2(4)3(5)6/h1H3,(H,5,6)
IUPAC Name
2-oxopropanoic acid
SMILES
CC(=O)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as alpha-keto acids and derivatives. These are organic compounds containing an aldehyde substituted with a keto group on the adjacent carbon.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassKeto acids and derivatives
Sub ClassAlpha-keto acids and derivatives
Direct ParentAlpha-keto acids and derivatives
Alternative Parents
Substituents
  • Alpha-keto acid
  • Alpha-hydroxy ketone
  • Ketone
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Aliphatic acyclic compound
Molecular FrameworkAliphatic acyclic compounds
External Descriptors
Pharmacology
IndicationFor nutritional supplementation, also for treating dietary shortage or imbalance
PharmacodynamicsPyruvic acid or pyruvate is a key intermediate in the glycolytic and pyruvate dehydrogenase pathways, which are involved in biological energy production. Pyruvate is widely found in living organisms. It is not an essential nutrient since it can be synthesized in the cells of the body. Certain fruits and vegetables are rich in pyruvate. For example, an average-size red apple contains approximately 450 milligrams. Dark beer and red wine are also rich sources of pyruvate. Recent research suggests that pyruvate in high concentrations may have a role in cardiovascular therapy, as an inotropic agent. Supplements of this dietary substance may also have bariatric and ergogenic applications.
Mechanism of actionPyruvate serves as a biological fuel by being converted to acetyl coenzyme A, which enters the tricarboxylic acid or Krebs cycle where it is metabolized to produce ATP aerobically. Energy can also be obtained anaerobically from pyruvate via its conversion to lactate. Pyruvate injections or perfusions increase contractile function of hearts when metabolizing glucose or fatty acids. This inotropic effect is striking in hearts stunned by ischemia/reperfusion. The inotropic effect of pyruvate requires intracoronary infusion. Among possible mechanisms for this effect are increased generation of ATP and an increase in ATP phosphorylation potential. Another is activation of pyruvate dehydrogenase, promoting its own oxidation by inhibiting pyruvate dehydrogenase kinase. Pyruvate dehydrogenase is inactivated in ischemia myocardium. Yet another is reduction of cytosolic inorganic phosphate concentration. Pyruvate, as an antioxidant, is known to scavenge such reactive oxygen species as hydrogen peroxide and lipid peroxides. Indirectly, supraphysiological levels of pyruvate may increase cellular reduced glutathione.
Related Articles
AbsorptionPyruvate is absorbed from the gastrointestinal tract from whence it is transported to the liver via the portal circulation.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

In the liver, pyruvate is metabolized via several pathways.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityThose taking large doses of supplemental pyruvate—usually greater than 5 grams daily—have reported gastrointestinal symptoms, including abdominal discomfort and bloating, gas and diarrhea. One child receiving pyruvate intravenously for restrictive cardiomyopathy died.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Cysteine MetabolismMetabolicSMP00013
Sialuria or French Type SialuriaDiseaseSMP00217
Pyruvate Carboxylase DeficiencyDiseaseSMP00350
Pyruvaldehyde DegradationMetabolicSMP00459
Primary hyperoxaluria II, PH2DiseaseSMP00558
Fructose-1,6-diphosphatase deficiencyDiseaseSMP00562
Succinic semialdehyde dehydrogenase deficiencyDiseaseSMP00567
Fanconi-bickel syndromeDiseaseSMP00572
3-Phosphoglycerate dehydrogenase deficiencyDiseaseSMP00721
Cystinosis, ocular nonnephropathicDiseaseSMP00722
The oncogenic action of FumarateDiseaseSMP02295
GluconeogenesisMetabolicSMP00128
Pyruvate Dehydrogenase Complex DeficiencyDiseaseSMP00212
Non Ketotic HyperglycinemiaDiseaseSMP00223
Salla Disease/Infantile Sialic Acid Storage DiseaseDiseaseSMP00240
Primary Hyperoxaluria Type IDiseaseSMP00352
ArgininemiaDiseaseSMP00357
Dimethylglycine Dehydrogenase DeficiencyDiseaseSMP00484
Glycogenosis, Type VII. Tarui diseaseDiseaseSMP00531
Congenital lactic acidosisDiseaseSMP00546
Fumarase deficiencyDiseaseSMP00547
Mitochondrial complex II deficiencyDiseaseSMP00548
Pyruvate dehydrogenase deficiency (E2)DiseaseSMP00551
Glycogenosis, Type IBDiseaseSMP00573
Glycogenosis, Type ICDiseaseSMP00574
Citrullinemia Type IDiseaseSMP00001
Carbamoyl Phosphate Synthetase DeficiencyDiseaseSMP00002
Amino Sugar MetabolismMetabolicSMP00045
Alanine MetabolismMetabolicSMP00055
Glutamate MetabolismMetabolicSMP00072
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9753
Blood Brain Barrier+0.9401
Caco-2 permeable-0.6934
P-glycoprotein substrateNon-substrate0.8153
P-glycoprotein inhibitor INon-inhibitor0.9498
P-glycoprotein inhibitor IINon-inhibitor0.9514
Renal organic cation transporterNon-inhibitor0.949
CYP450 2C9 substrateNon-substrate0.7951
CYP450 2D6 substrateNon-substrate0.9402
CYP450 3A4 substrateNon-substrate0.7806
CYP450 1A2 substrateNon-inhibitor0.98
CYP450 2C9 inhibitorNon-inhibitor0.9608
CYP450 2D6 inhibitorNon-inhibitor0.9697
CYP450 2C19 inhibitorNon-inhibitor0.9834
CYP450 3A4 inhibitorNon-inhibitor0.9882
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9932
Ames testNon AMES toxic0.8578
CarcinogenicityCarcinogens 0.5171
BiodegradationReady biodegradable0.9262
Rat acute toxicity1.7859 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9883
hERG inhibition (predictor II)Non-inhibitor0.9801
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateLiquid
Experimental Properties
PropertyValueSource
melting point13.8 °CPhysProp
boiling point54 °C at 1.00E+01 mm HgPhysProp
water solubility1E+006 mg/L (at 20 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP-0.5Not Available
pKa2.45 (at 25 °C)KORTUM,G ET AL (1961)
Predicted Properties
PropertyValueSource
Water Solubility134.0 mg/mLALOGPS
logP-0.38ALOGPS
logP0.066ChemAxon
logS0.18ALOGPS
pKa (Strongest Acidic)2.93ChemAxon
pKa (Strongest Basic)-9.6ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area54.37 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity17.99 m3·mol-1ChemAxon
Polarizability7.31 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.4 KB)
Spectra
Spectrum TypeDescriptionSplash Key
GC-MSGC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies)splash10-00dr-4900000000-f26ef76666e40ab9fe61View in MoNA
GC-MSGC-MS Spectrum - GC-MS (1 MEOX; 1 TMS)splash10-00di-5900000000-b8e81f82572d4796e944View in MoNA
GC-MSGC-MS Spectrum - GC-MS (2 TMS)splash10-014i-5970000000-154bf9ad168a12593fccView in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (HITACHI M-80B) , Positivesplash10-0006-9000000000-a2cf85a5e1d2379d26dfView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 10V, Negativesplash10-000i-9000000000-dd49835da8355fb6e625View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 20V, Negativesplash10-000i-9000000000-f09d8e3d7a774b255d89View in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 30V, Negativesplash10-0006-9000000000-7d91f6f626cab1a366fdView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 40V, Negativesplash10-0006-9000000000-8ae98cdb3e142034e52aView in MoNA
LC-MS/MSLC-MS/MS Spectrum - LC-ESI-QQ (API3000, Applied Biosystems) 50V, Negativesplash10-0006-9000000000-e04e6c68013983e1b6dcView in MoNA
MSMass Spectrum (Electron Ionization)splash10-0006-9000000000-f315d0752893e7d0c657View in MoNA
1D NMR13C NMR SpectrumNot Available
1D NMR1H NMR SpectrumNot Available
1D NMR1H NMR SpectrumNot Available
1D NMR13C NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

Tadamitsu Kiyoura, “Process for producing salts of pyruvic acid.” U.S. Patent US4242525, issued December, 1965.

US4242525
General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSDownload (72 KB)
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-linked monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate (By similarity).
Gene Name:
SLC16A3
Uniprot ID:
O15427
Molecular Weight:
49468.9 Da
References
  1. Shimada A, Nakagawa Y, Morishige H, Yamamoto A, Fujita T: Functional characteristics of H+ -dependent nicotinate transport in primary cultures of astrocytes from rat cerebral cortex. Neurosci Lett. 2006 Jan 16;392(3):207-12. Epub 2005 Oct 5. [PubMed:16213084 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Transporter activity
Specific Function:
Very active and specific thyroid hormone transporter. Stimulates cellular uptake of thyroxine (T4), triiodothyronine (T3), reverse triiodothyronine (rT3) and diidothyronine. Does not transport Leu, Phe, Trp or Tyr.
Gene Name:
SLC16A2
Uniprot ID:
P36021
Molecular Weight:
59510.86 Da
References
  1. Bonen A, Heynen M, Hatta H: Distribution of monocarboxylate transporters MCT1-MCT8 in rat tissues and human skeletal muscle. Appl Physiol Nutr Metab. 2006 Feb;31(1):31-9. [PubMed:16604139 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Pyridoxal phosphate binding
Specific Function:
Can metabolize asymmetric dimethylarginine (ADMA) via transamination to alpha-keto-delta-(NN-dimethylguanidino) valeric acid (DMGV). ADMA is a potent inhibitor of nitric-oxide (NO) synthase, and this activity provides mechanism through which the kidney regulates blood pressure.
Gene Name:
AGXT2
Uniprot ID:
Q9BYV1
Molecular Weight:
57155.905 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Tamaki N, Fujimoto S, Mizota C, Kaneko M, Kikugawa M: Inhibitory effect of 6-azauracil on beta-alanine metabolism in rat. J Nutr Sci Vitaminol (Tokyo). 1989 Oct;35(5):451-61. [PubMed:2632679 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-linked monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate (By similarity).
Gene Name:
SLC16A5
Uniprot ID:
O15375
Molecular Weight:
54993.04 Da
References
  1. Bonen A, Heynen M, Hatta H: Distribution of monocarboxylate transporters MCT1-MCT8 in rat tissues and human skeletal muscle. Appl Physiol Nutr Metab. 2006 Feb;31(1):31-9. [PubMed:16604139 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Pyruvate kinase activity
Specific Function:
Plays a key role in glycolysis.
Gene Name:
PKLR
Uniprot ID:
P30613
Molecular Weight:
61829.575 Da
References
  1. Percy MJ, van Wijk R, Haggan S, Savage GA, Boyd K, Dempsey S, Hamilton J, Kettle P, Kyle A, Shepherd CW, van Solinge WW, Lappin TR, McMullin MF: Pyruvate kinase deficient hemolytic anemia in the Northern Irish population. Blood Cells Mol Dis. 2007 Sep-Oct;39(2):189-94. Epub 2007 Jun 15. [PubMed:17574881 ]
  2. Meza NW, Quintana-Bustamante O, Puyet A, Rio P, Navarro S, Diez A, Bueren JA, Bautista JM, Segovia JC: In vitro and in vivo expression of human erythrocyte pyruvate kinase in erythroid cells: a gene therapy approach. Hum Gene Ther. 2007 Jun;18(6):502-14. [PubMed:17547515 ]
  3. Rajaseger G, Lim CL, Lee KW, Arjunan P, Jia L, Moochhala S: Profiling of hepatocellular proteins by 1D PAGE-MALDI/MS/MS in a rat heat stress model. Front Biosci. 2006 Sep 1;11:2924-8. [PubMed:16720364 ]
  4. Xu J, Christian B, Jump DB: Regulation of rat hepatic L-pyruvate kinase promoter composition and activity by glucose, n-3 polyunsaturated fatty acids, and peroxisome proliferator-activated receptor-alpha agonist. J Biol Chem. 2006 Jul 7;281(27):18351-62. Epub 2006 Apr 27. [PubMed:16644726 ]
  5. Suzuki T, Kawamoto M, Murai A, Muramatsu T: Identification of the regulatory region of the L-type pyruvate kinase gene in mouse liver by hydrodynamics-based gene transfection. J Nutr. 2006 Jan;136(1):16-20. [PubMed:16365052 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-linked monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate (By similarity).
Gene Name:
SLC16A6
Uniprot ID:
O15403
Molecular Weight:
57392.83 Da
References
  1. Bonen A, Heynen M, Hatta H: Distribution of monocarboxylate transporters MCT1-MCT8 in rat tissues and human skeletal muscle. Appl Physiol Nutr Metab. 2006 Feb;31(1):31-9. [PubMed:16604139 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-coupled monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate. Functions as high-affinity pyruvate transporter.
Gene Name:
SLC16A7
Uniprot ID:
O60669
Molecular Weight:
52199.745 Da
References
  1. Bonen A, Heynen M, Hatta H: Distribution of monocarboxylate transporters MCT1-MCT8 in rat tissues and human skeletal muscle. Appl Physiol Nutr Metab. 2006 Feb;31(1):31-9. [PubMed:16604139 ]
  2. Hinoi E, Takarada T, Tsuchihashi Y, Fujimori S, Moriguchi N, Wang L, Uno K, Yoneda Y: A molecular mechanism of pyruvate protection against cytotoxicity of reactive oxygen species in osteoblasts. Mol Pharmacol. 2006 Sep;70(3):925-35. Epub 2006 Jun 9. [PubMed:16766717 ]
  3. 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. [PubMed:17556391 ]
  4. de Laplanche E, Gouget K, Cleris G, Dragounoff F, Demont J, Morales A, Bezin L, Godinot C, Perriere G, Mouchiroud D, Simonnet H: Physiological oxygenation status is required for fully differentiated phenotype in kidney cortex proximal tubules. Am J Physiol Renal Physiol. 2006 Oct;291(4):F750-60. Epub 2006 Apr 4. [PubMed:16597615 ]
  5. Pierre K, Pellerin L: Monocarboxylate transporters in the central nervous system: distribution, regulation and function. J Neurochem. 2005 Jul;94(1):1-14. [PubMed:15953344 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Pyruvate dehydrogenase activity
Specific Function:
The pyruvate dehydrogenase complex catalyzes the overall conversion of pyruvate to acetyl-CoA and CO(2), and thereby links the glycolytic pathway to the tricarboxylic cycle.
Gene Name:
PDHB
Uniprot ID:
P11177
Molecular Weight:
39233.1 Da
References
  1. Kumar V, Rangaraj N, Shivaji S: Activity of pyruvate dehydrogenase A (PDHA) in hamster spermatozoa correlates positively with hyperactivation and is associated with sperm capacitation. Biol Reprod. 2006 Nov;75(5):767-77. Epub 2006 Jul 19. [PubMed:16855207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Pyruvate kinase activity
Specific Function:
Glycolytic enzyme that catalyzes the transfer of a phosphoryl group from phosphoenolpyruvate (PEP) to ADP, generating ATP. Stimulates POU5F1-mediated transcriptional activation. Plays a general role in caspase independent cell death of tumor cells. The ratio betwween the highly active tetrameric form and nearly inactive dimeric form determines whether glucose carbons are channeled to biosynthet...
Gene Name:
PKM
Uniprot ID:
P14618
Molecular Weight:
57936.38 Da
References
  1. Li Y, Chang Y, Zhang L, Feng Q, Liu Z, Zhang Y, Zuo J, Meng Y, Fang F: High glucose upregulates pantothenate kinase 4 (PanK4) and thus affects M2-type pyruvate kinase (Pkm2). Mol Cell Biochem. 2005 Sep;277(1-2):117-25. [PubMed:16132722 ]
  2. Stetak A, Veress R, Ovadi J, Csermely P, Keri G, Ullrich A: Nuclear translocation of the tumor marker pyruvate kinase M2 induces programmed cell death. Cancer Res. 2007 Feb 15;67(4):1602-8. [PubMed:17308100 ]
  3. Vlaeminck-Guillem V, Safi R, Guillem P, Leteurtre E, Duterque-Coquillaud M, Laudet V: Thyroid hormone receptor expression in the obligatory paedomorphic salamander Necturus maculosus. Int J Dev Biol. 2006;50(6):553-60. [PubMed:16741870 ]
  4. Weinberger R, Appel B, Stein A, Metz Y, Neheman A, Barak M: The pyruvate kinase isoenzyme M2 (Tu M2-PK) as a tumour marker for renal cell carcinoma. Eur J Cancer Care (Engl). 2007 Jul;16(4):333-7. [PubMed:17587357 ]
  5. Staib P, Hoffmann M, Schinkothe T: Plasma levels of tumor M2-pyruvate kinase should not be used as a tumor marker for hematological malignancies and solid tumors. Clin Chem Lab Med. 2006;44(1):28-31. [PubMed:16375581 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Succinate-semialdehyde dehydrogenase binding
Specific Function:
Catalyzes the conversion of gamma-aminobutyrate and L-beta-aminoisobutyrate to succinate semialdehyde and methylmalonate semialdehyde, respectively. Can also convert delta-aminovalerate and beta-alanine.
Gene Name:
ABAT
Uniprot ID:
P80404
Molecular Weight:
56438.405 Da
References
  1. Andersen G, Andersen B, Dobritzsch D, Schnackerz KD, Piskur J: A gene duplication led to specialized gamma-aminobutyrate and beta-alanine aminotransferase in yeast. FEBS J. 2007 Apr;274(7):1804-17. Epub 2007 Mar 12. [PubMed:17355287 ]
  2. Schmidt C, Hofmann U, Kohlmuller D, Murdter T, Zanger UM, Schwab M, Hoffmann GF: Comprehensive analysis of pyrimidine metabolism in 450 children with unspecific neurological symptoms using high-pressure liquid chromatography-electrospray ionization tandem mass spectrometry. J Inherit Metab Dis. 2005;28(6):1109-22. [PubMed:16435204 ]
  3. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-linked monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate (By similarity).
Gene Name:
SLC16A4
Uniprot ID:
O15374
Molecular Weight:
54021.43 Da
References
  1. Kay HH, Zhu S, Tsoi S: Hypoxia and lactate production in trophoblast cells. Placenta. 2007 Aug-Sep;28(8-9):854-60. Epub 2007 Feb 2. [PubMed:17275903 ]
  2. Han M, Trotta P, Coleman C, Linask KK: MCT-4, A511/Basigin and EF5 expression patterns during early chick cardiomyogenesis indicate cardiac cell differentiation occurs in a hypoxic environment. Dev Dyn. 2006 Jan;235(1):124-31. [PubMed:16110503 ]
  3. Bonen A, Heynen M, Hatta H: Distribution of monocarboxylate transporters MCT1-MCT8 in rat tissues and human skeletal muscle. Appl Physiol Nutr Metab. 2006 Feb;31(1):31-9. [PubMed:16604139 ]
  4. Pierre K, Pellerin L: Monocarboxylate transporters in the central nervous system: distribution, regulation and function. J Neurochem. 2005 Jul;94(1):1-14. [PubMed:15953344 ]
  5. Shimada A, Nakagawa Y, Morishige H, Yamamoto A, Fujita T: Functional characteristics of H+ -dependent nicotinate transport in primary cultures of astrocytes from rat cerebral cortex. Neurosci Lett. 2006 Jan 16;392(3):207-12. Epub 2005 Oct 5. [PubMed:16213084 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-linked monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate (By similarity).
Gene Name:
SLC16A8
Uniprot ID:
O95907
Molecular Weight:
52318.215 Da
References
  1. Jansen S, Esmaeilpour T, Pantaleon M, Kaye PL: Glucose affects monocarboxylate cotransporter (MCT) 1 expression during mouse preimplantation development. Reproduction. 2006 Mar;131(3):469-79. [PubMed:16514190 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Symporter activity
Specific Function:
Proton-coupled monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate. Depending on the tissue and on cicumstances, mediates the import or export of lactic acid and ketone bod...
Gene Name:
SLC16A1
Uniprot ID:
P53985
Molecular Weight:
53943.685 Da
References
  1. Duerr JM, Tucker K: Pyruvate transport in isolated cardiac mitochondria from two species of amphibian exhibiting dissimilar aerobic scope: Bufo marinus and Rana catesbeiana. J Exp Zool A Ecol Genet Physiol. 2007 Aug 1;307(8):425-38. [PubMed:17583564 ]
  2. Han M, Trotta P, Coleman C, Linask KK: MCT-4, A511/Basigin and EF5 expression patterns during early chick cardiomyogenesis indicate cardiac cell differentiation occurs in a hypoxic environment. Dev Dyn. 2006 Jan;235(1):124-31. [PubMed:16110503 ]
  3. Shimoyama Y, Akihara Y, Kirat D, Iwano H, Hirayama K, Kagawa Y, Ohmachi T, Matsuda K, Okamoto M, Kadosawa T, Yokota H, Taniyama H: Expression of monocarboxylate transporter 1 in oral and ocular canine melanocytic tumors. Vet Pathol. 2007 Jul;44(4):449-57. [PubMed:17606506 ]
  4. Shimada A, Nakagawa Y, Morishige H, Yamamoto A, Fujita T: Functional characteristics of H+ -dependent nicotinate transport in primary cultures of astrocytes from rat cerebral cortex. Neurosci Lett. 2006 Jan 16;392(3):207-12. Epub 2005 Oct 5. [PubMed:16213084 ]
  5. Philp A, Macdonald AL, Watt PW: Lactate--a signal coordinating cell and systemic function. J Exp Biol. 2005 Dec;208(Pt 24):4561-75. [PubMed:16326938 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Pyruvate carboxylase activity
Specific Function:
Pyruvate carboxylase catalyzes a 2-step reaction, involving the ATP-dependent carboxylation of the covalently attached biotin in the first step and the transfer of the carboxyl group to pyruvate in the second. Catalyzes in a tissue specific manner, the initial reactions of glucose (liver, kidney) and lipid (adipose tissue, liver, brain) synthesis from pyruvate.
Gene Name:
PC
Uniprot ID:
P11498
Molecular Weight:
129632.565 Da
References
  1. Jitrapakdee S, Vidal-Puig A, Wallace JC: Anaplerotic roles of pyruvate carboxylase in mammalian tissues. Cell Mol Life Sci. 2006 Apr;63(7-8):843-54. [PubMed:16505973 ]
  2. Simpson NE, Khokhlova N, Oca-Cossio JA, Constantinidis I: Insights into the role of anaplerosis in insulin secretion: A 13C NMR study. Diabetologia. 2006 Jun;49(6):1338-48. Epub 2006 Mar 31. [PubMed:16575559 ]
  3. Jensen MV, Joseph JW, Ilkayeva O, Burgess S, Lu D, Ronnebaum SM, Odegaard M, Becker TC, Sherry AD, Newgard CB: Compensatory responses to pyruvate carboxylase suppression in islet beta-cells. Preservation of glucose-stimulated insulin secretion. J Biol Chem. 2006 Aug 4;281(31):22342-51. Epub 2006 Jun 1. [PubMed:16740637 ]
  4. Ikeda K, Yukihiro Hiraoka B, Iwai H, Matsumoto T, Mineki R, Taka H, Takamori K, Ogawa H, Yamakura F: Detection of 6-nitrotryptophan in proteins by Western blot analysis and its application for peroxynitrite-treated PC12 cells. Nitric Oxide. 2007 Feb;16(1):18-28. Epub 2006 May 4. [PubMed:16765071 ]
  5. Liu L, Li Y, Zhu Y, Du G, Chen J: Redistribution of carbon flux in Torulopsis glabrata by altering vitamin and calcium level. Metab Eng. 2007 Jan;9(1):21-9. Epub 2006 Aug 12. [PubMed:17008113 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Symporter activity
Specific Function:
Proton-coupled monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate. Functions as high-affinity pyruvate transporter.
Gene Name:
SLC16A7
Uniprot ID:
O60669
Molecular Weight:
52199.745 Da
References
  1. Broer S, Broer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW: Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes. Biochem J. 1999 Aug 1;341 ( Pt 3):529-35. [PubMed:10417314 ]
  2. Lin RY, Vera JC, Chaganti RS, Golde DW: Human monocarboxylate transporter 2 (MCT2) is a high affinity pyruvate transporter. J Biol Chem. 1998 Oct 30;273(44):28959-65. [PubMed:9786900 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Symporter activity
Specific Function:
Proton-coupled monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate. Depending on the tissue and on cicumstances, mediates the import or export of lactic acid and ketone bod...
Gene Name:
SLC16A1
Uniprot ID:
P53985
Molecular Weight:
53943.685 Da
References
  1. Broer S, Rahman B, Pellegri G, Pellerin L, Martin JL, Verleysdonk S, Hamprecht B, Magistretti PJ: Comparison of lactate transport in astroglial cells and monocarboxylate transporter 1 (MCT 1) expressing Xenopus laevis oocytes. Expression of two different monocarboxylate transporters in astroglial cells and neurons. J Biol Chem. 1997 Nov 28;272(48):30096-102. [PubMed:9374487 ]
  2. Broer S, Schneider HP, Broer A, Rahman B, Hamprecht B, Deitmer JW: Characterization of the monocarboxylate transporter 1 expressed in Xenopus laevis oocytes by changes in cytosolic pH. Biochem J. 1998 Jul 1;333 ( Pt 1):167-74. [PubMed:9639576 ]
  3. Lin RY, Vera JC, Chaganti RS, Golde DW: Human monocarboxylate transporter 2 (MCT2) is a high affinity pyruvate transporter. J Biol Chem. 1998 Oct 30;273(44):28959-65. [PubMed:9786900 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Transporter activity
Specific Function:
Sodium-independent transporter that mediates the update of aromatic acid. Can function as a net efflux pathway for aromatic amino acids in the basosolateral epithelial cells (By similarity).
Gene Name:
SLC16A10
Uniprot ID:
Q8TF71
Molecular Weight:
55492.07 Da
References
  1. Kim DK, Kanai Y, Chairoungdua A, Matsuo H, Cha SH, Endou H: Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters. J Biol Chem. 2001 May 18;276(20):17221-8. Epub 2001 Feb 20. [PubMed:11278508 ]
  2. Kim DK, Kanai Y, Matsuo H, Kim JY, Chairoungdua A, Kobayashi Y, Enomoto A, Cha SH, Goya T, Endou H: The human T-type amino acid transporter-1: characterization, gene organization, and chromosomal location. Genomics. 2002 Jan;79(1):95-103. [PubMed:11827462 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
May mediate the release of newly synthesized prostaglandins from cells, the transepithelial transport of prostaglandins, and the clearance of prostaglandins from the circulation. Transports PGD2, as well as PGE1, PGE2 and PGF2A.
Gene Name:
SLCO2A1
Uniprot ID:
Q92959
Molecular Weight:
70043.33 Da
References
  1. Chan BS, Endo S, Kanai N, Schuster VL: Identification of lactate as a driving force for prostanoid transport by prostaglandin transporter PGT. Am J Physiol Renal Physiol. 2002 Jun;282(6):F1097-102. [PubMed:11997326 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Symporter activity
Specific Function:
Proton-linked monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucine, valine and isoleucine, and the ketone bodies acetoacetate, beta-hydroxybutyrate and acetate (By similarity).
Gene Name:
SLC16A3
Uniprot ID:
O15427
Molecular Weight:
49468.9 Da
References
  1. Manning Fox JE, Meredith D, Halestrap AP: Characterisation of human monocarboxylate transporter 4 substantiates its role in lactic acid efflux from skeletal muscle. J Physiol. 2000 Dec 1;529 Pt 2:285-93. [PubMed:11101640 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23