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Identification
NameEdetic Acid
Accession NumberDB00974  (APRD01327)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

A chelating agent (chelating agents) that sequesters a variety of polyvalent cations. It is used in pharmaceutical manufacturing and as a food additive. [PubChem]

Structure
Thumb
Synonyms
(ethylenedinitrilo)tetraacetic acid, ion(4−)
{[-(bis-carboxymethyl-amino)-ethyl]-carboxymethyl-amino}-acetic acid
2,2',2'',2'''-(ethane-1,2-diyldinitrilo)tetraacetate
acide edetique
Acide ethylenediaminetetracetique
Acido edetico
Acidum edeticum
EDTA
EDTA, ion(4-)
Ethylenediaminetetraacetate
Ethylenediaminetetraacetic acid
N,N'-1,2-Ethane diylbis-(N-(carboxymethyl)glycine)
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Calcium Disodium Versenateinjection200 mg/mLintramuscular; intravenousMedicis Pharmaceutical Corp2013-06-212016-04-05Us
Calcium Disodium Versenateinjection200 mg/mLintramuscularGraceway Pharmaceuticals, LLC2009-07-092015-12-31Us
Calcium Disodium Versenateinjection200 mg/mLintramuscular3 M Pharmaceuticals2009-07-092015-12-31Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
CheladratePharmex
Diso-TateO'Neal, Jones
EndrateBersworth
Uni WashUnited
Brand mixtures
NameLabellerIngredients
Foam Care Pcmx Surgical Hand ScrubBallard Medical Products
Salts
Name/CASStructureProperties
Disodium edetate dihydrate
6381-92-6
Thumb
  • InChI Key: OVBJJZOQPCKUOR-UHFFFAOYSA-L
  • Monoisotopic Mass: 372.075684156
  • Average Mass: 372.2369
DBSALT001820
Edetate calcium disodium
62-33-9
Thumb
  • InChI Key: SHWNNYZBHZIQQV-UHFFFAOYSA-J
  • Monoisotopic Mass: 374.001495875
  • Average Mass: 374.268
DBSALT000837
Edetate copper disodium
14025-15-1
Thumb
  • InChI Key: KCFCAUKZKOSSBI-UHFFFAOYSA-J
  • Monoisotopic Mass: 396.968502
  • Average Mass: 397.738
DBSALT001713
Edetate disodium
139-33-3
Thumb
  • InChI Key: ZGTMUACCHSMWAC-UHFFFAOYSA-L
  • Monoisotopic Mass: 336.054554784
  • Average Mass: 336.2063
DBSALT000838
Categories
UNII8U5D034955
CAS number60-00-4
WeightAverage: 292.2426
Monoisotopic: 292.090665498
Chemical FormulaC10H16N2O8
InChI KeyKCXVZYZYPLLWCC-UHFFFAOYSA-N
InChI
InChI=1S/C10H16N2O8/c13-7(14)3-11(4-8(15)16)1-2-12(5-9(17)18)6-10(19)20/h1-6H2,(H,13,14)(H,15,16)(H,17,18)(H,19,20)
IUPAC Name
2-({2-[bis(carboxymethyl)amino]ethyl}(carboxymethyl)amino)acetic acid
SMILES
OC(=O)CN(CCN(CC(O)=O)CC(O)=O)CC(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as tetracarboxylic acids and derivatives. These are carboxylic acids containing exactly four carboxyl groups.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassTetracarboxylic acids and derivatives
Direct ParentTetracarboxylic acids and derivatives
Alternative Parents
Substituents
  • Tetracarboxylic acid or derivatives
  • Alpha-amino acid or derivatives
  • Alpha-amino acid
  • Tertiary aliphatic amine
  • Tertiary amine
  • Carboxylic acid
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aliphatic acyclic compound
Molecular FrameworkAliphatic acyclic compounds
External Descriptors
Pharmacology
IndicationFor the reduction of blood levels and depot stores of lead in lead poisoning (acute and chronic) and lead encephalopathy, in both pediatric populations and adults.
PharmacodynamicsEdetate calcium is a heavy metal chelating agent. The calcium in edetate calcium can be displaced by divalent or trivalent metals to form a stable water soluble complex that can be excreted in the urine. In theory, 1 g of edetate calcium can theoretically bind 620 mg of lead, but in reality only about 5 mg per gram is actually excreted into the urine in lead poisoned patients. In addition to chelating lead, edetate calcium also chelates and eliminates zinc from the body. Edetate calcium also binds cadmium, copper, iron and manganese, but to a much lesser extent than either lead or zinc. Edetate calcium is relatively ineffective for use in treating mercury, gold or arsenic poisoning.
Mechanism of actionThe pharmacologic effects of edetate calcium disodium are due to the formation of chelates with divalent and trivalent metals. A stable chelate will form with any metal that has the ability to displace calcium from the molecule, a feature shared by lead, zinc, cadmium, manganese, iron and mercury. The amounts of manganese and iron metabolized are not significant. Copper is not mobilized and mercury is unavailable for chelation because it is too tightly bound to body ligands or it is stored in inaccessible body compartments. The excretion of calcium by the body is not increased following intravenous administration of edetate calcium disodium, but the excretion of zinc is considerably increased.
Related Articles
AbsorptionPoorly absorbed from the gastrointestinal tract. Well absorbed following intramuscular injection.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Almost none of the compound is metabolized.

Route of eliminationIt is excreted primarily by the kidney, with about 50% excreted in one hour and over 95% within 24 hours.2 Almost none of the compound is metabolized.
Half lifeThe half life of edetate calcium disodium is 20 to 60 minutes.
ClearanceNot Available
ToxicityInadvertent administration of 5 times the recommended dose, infused intravenously over a 24 hour period, to an asymptomatic 16 month old patient with a blood lead content of 56 mcg/dl did not cause any ill effects. Edetate calcium disodium can aggravate the symptoms of severe lead poisoning, therefore, most toxic effects (cerebral edema, renal tubular necrosis) appear to be associated with lead poisoning. Because of cerebral edema, a therapeutic dose may be lethal to an adult or a pediatric patient with lead encephalopathy. Higher dosage of edetate calcium disodium may produce a more severe zinc deficiency.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8668
Blood Brain Barrier-0.7126
Caco-2 permeable-0.5739
P-glycoprotein substrateSubstrate0.6377
P-glycoprotein inhibitor INon-inhibitor0.9296
P-glycoprotein inhibitor IINon-inhibitor0.972
Renal organic cation transporterNon-inhibitor0.8473
CYP450 2C9 substrateNon-substrate0.8457
CYP450 2D6 substrateNon-substrate0.8271
CYP450 3A4 substrateNon-substrate0.7616
CYP450 1A2 substrateNon-inhibitor0.8959
CYP450 2C9 inhibitorNon-inhibitor0.9225
CYP450 2D6 inhibitorNon-inhibitor0.9306
CYP450 2C19 inhibitorNon-inhibitor0.9174
CYP450 3A4 inhibitorNon-inhibitor0.9288
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9891
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7715
BiodegradationNot ready biodegradable0.8307
Rat acute toxicity1.8974 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8158
hERG inhibition (predictor II)Non-inhibitor0.9341
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Graceway pharmaceuticals llc
  • Watson laboratories inc
  • 3m pharmaceuticals inc
Packagers
Dosage forms
FormRouteStrength
Injectionintramuscular200 mg/mL
Injectionintramuscular; intravenous200 mg/mL
Liquidtopical
Prices
Unit descriptionCostUnit
Endrate 150 mg/ml ampul1.44USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point237 °CNot Available
water solubility1000000 mg/L at 25 °CMEYLAN,WM et al. (1996)
logP-2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility9.26 mg/mLALOGPS
logP-1.2ALOGPS
logP-5.2ChemAxon
logS-1.5ALOGPS
pKa (Strongest Acidic)1.49ChemAxon
pKa (Strongest Basic)8.13ChemAxon
Physiological Charge-3ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area155.68 Å2ChemAxon
Rotatable Bond Count11ChemAxon
Refractivity62.35 m3·mol-1ChemAxon
Polarizability25.64 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10.2 KB)
Spectra
Spectrum TypeDescriptionSplash Key
GC-MSGC-MS Spectrum - GC-MS (4 TMS)splash10-9zr4100000-52370879752b5b63ccc2View in MoNA
References
Synthesis Reference

Bersworth, F.C.; U.S. Patent 2,407,645; September 17,1946; assigned to The Martin Dennis Co.

General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AbciximabAbciximab may increase the anticoagulant activities of Edetic Acid.
AcenocoumarolEdetic Acid may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Edetic Acid.
AlteplaseAlteplase may increase the anticoagulant activities of Edetic Acid.
Aminosalicylic AcidAminosalicylic Acid may increase the anticoagulant activities of Edetic Acid.
AnagrelideAnagrelide may increase the anticoagulant activities of Edetic Acid.
ApixabanApixaban may increase the anticoagulant activities of Edetic Acid.
ArgatrobanEdetic Acid may increase the anticoagulant activities of Argatroban.
Bismuth SubsalicylateBismuth Subsalicylate may increase the anticoagulant activities of Edetic Acid.
BivalirudinEdetic Acid may increase the anticoagulant activities of Bivalirudin.
CaffeineCaffeine may increase the anticoagulant activities of Edetic Acid.
CangrelorCangrelor may increase the anticoagulant activities of Edetic Acid.
CelecoxibCelecoxib may increase the anticoagulant activities of Edetic Acid.
CilostazolCilostazol may increase the anticoagulant activities of Edetic Acid.
CitalopramCitalopram may increase the anticoagulant activities of Edetic Acid.
ClopidogrelClopidogrel may increase the anticoagulant activities of Edetic Acid.
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Collagenase clostridium histolyticum.
Cyproterone acetateThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Cyproterone acetate.
Dabigatran etexilateDabigatran etexilate may increase the anticoagulant activities of Edetic Acid.
DalteparinEdetic Acid may increase the anticoagulant activities of Dalteparin.
DanaparoidEdetic Acid may increase the anticoagulant activities of Danaparoid.
DasatinibDasatinib may increase the anticoagulant activities of Edetic Acid.
DeferasiroxThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Deferasirox.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Deoxycholic Acid.
DesirudinEdetic Acid may increase the anticoagulant activities of Desirudin.
DesogestrelDesogestrel may decrease the anticoagulant activities of Edetic Acid.
DesvenlafaxineDesvenlafaxine may increase the anticoagulant activities of Edetic Acid.
DiclofenacDiclofenac may increase the anticoagulant activities of Edetic Acid.
DienogestThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Dienogest.
DiflunisalDiflunisal may increase the anticoagulant activities of Edetic Acid.
DihydrocodeineDihydrocodeine may increase the anticoagulant activities of Edetic Acid.
DipyridamoleDipyridamole may increase the anticoagulant activities of Edetic Acid.
DrospirenoneDrospirenone may decrease the anticoagulant activities of Edetic Acid.
DuloxetineDuloxetine may increase the anticoagulant activities of Edetic Acid.
EdoxabanEdoxaban may increase the anticoagulant activities of Edetic Acid.
EnoxaparinEdetic Acid may increase the anticoagulant activities of Enoxaparin.
EpoprostenolThe risk or severity of adverse effects can be increased when Epoprostenol is combined with Edetic Acid.
EptifibatideEptifibatide may increase the anticoagulant activities of Edetic Acid.
EscitalopramEscitalopram may increase the anticoagulant activities of Edetic Acid.
EstradiolEstradiol may decrease the anticoagulant activities of Edetic Acid.
EstropipateEstropipate may decrease the anticoagulant activities of Edetic Acid.
Ethinyl EstradiolEthinyl Estradiol may decrease the anticoagulant activities of Edetic Acid.
Ethynodiol diacetateEthynodiol may decrease the anticoagulant activities of Edetic Acid.
EtodolacEtodolac may increase the anticoagulant activities of Edetic Acid.
EtonogestrelThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Etonogestrel.
FenoprofenFenoprofen may increase the anticoagulant activities of Edetic Acid.
FloctafenineFloctafenine may increase the anticoagulant activities of Edetic Acid.
FluoxetineFluoxetine may increase the anticoagulant activities of Edetic Acid.
FlurbiprofenFlurbiprofen may increase the anticoagulant activities of Edetic Acid.
FluvoxamineFluvoxamine may increase the anticoagulant activities of Edetic Acid.
Fondaparinux sodiumEdetic Acid may increase the anticoagulant activities of Fondaparinux sodium.
HeparinEdetic Acid may increase the anticoagulant activities of Heparin.
Hydroxyprogesterone caproateThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Hydroxyprogesterone caproate.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Edetic Acid.
IbuprofenIbuprofen may increase the anticoagulant activities of Edetic Acid.
IcosapentIcosapent may increase the anticoagulant activities of Edetic Acid.
Icosapent ethylIcosapent ethyl may increase the anticoagulant activities of Edetic Acid.
IloprostThe risk or severity of adverse effects can be increased when Iloprost is combined with Edetic Acid.
IndomethacinIndomethacin may increase the anticoagulant activities of Edetic Acid.
Insulin AspartEdetic Acid may increase the hypoglycemic activities of Insulin Aspart.
Insulin DegludecEdetic Acid may increase the hypoglycemic activities of Insulin degludec.
Insulin DetemirEdetic Acid may increase the hypoglycemic activities of Insulin Detemir.
Insulin GlargineEdetic Acid may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineEdetic Acid may increase the hypoglycemic activities of Insulin Glulisine.
Insulin HumanEdetic Acid may increase the hypoglycemic activities of Insulin Regular.
Insulin LisproEdetic Acid may increase the hypoglycemic activities of Insulin Lispro.
KetoprofenKetoprofen may increase the anticoagulant activities of Edetic Acid.
KetorolacKetorolac may increase the anticoagulant activities of Edetic Acid.
LevomilnacipranLevomilnacipran may increase the anticoagulant activities of Edetic Acid.
LevonorgestrelThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Levonorgestrel.
Magnesium salicylateMagnesium salicylate may increase the anticoagulant activities of Edetic Acid.
Medroxyprogesterone AcetateThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Medroxyprogesterone Acetate.
Mefenamic acidMefenamic acid may increase the anticoagulant activities of Edetic Acid.
Megestrol acetateThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Megestrol acetate.
MeloxicamMeloxicam may increase the anticoagulant activities of Edetic Acid.
MestranolMestranol may decrease the anticoagulant activities of Edetic Acid.
MilnacipranMilnacipran may increase the anticoagulant activities of Edetic Acid.
NabumetoneNabumetone may increase the anticoagulant activities of Edetic Acid.
NadroparinEdetic Acid may increase the anticoagulant activities of Nadroparin.
NaproxenNaproxen may increase the anticoagulant activities of Edetic Acid.
NintedanibThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Nintedanib.
NorethisteroneThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Norethindrone.
NorgestimateNorgestimate may decrease the anticoagulant activities of Edetic Acid.
ObinutuzumabThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Obinutuzumab.
Omega-3 fatty acidsOmega-3 fatty acids may increase the anticoagulant activities of Edetic Acid.
Omega-3-acid ethyl estersOmega-3-acid ethyl esters may increase the anticoagulant activities of Edetic Acid.
OxaprozinOxaprozin may increase the anticoagulant activities of Edetic Acid.
ParoxetineParoxetine may increase the anticoagulant activities of Edetic Acid.
Pentosan PolysulfatePentosan Polysulfate may increase the anticoagulant activities of Edetic Acid.
PiroxicamPiroxicam may increase the anticoagulant activities of Edetic Acid.
PrasugrelPrasugrel may increase the anticoagulant activities of Edetic Acid.
ProgesteroneThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Progesterone.
ReteplaseReteplase may increase the anticoagulant activities of Edetic Acid.
RivaroxabanEdetic Acid may increase the anticoagulant activities of Rivaroxaban.
SalsalateSalsalate may increase the anticoagulant activities of Edetic Acid.
SertralineSertraline may increase the anticoagulant activities of Edetic Acid.
SulindacSulindac may increase the anticoagulant activities of Edetic Acid.
TenecteplaseTenecteplase may increase the anticoagulant activities of Edetic Acid.
Tiaprofenic acidTiaprofenic acid may increase the anticoagulant activities of Edetic Acid.
TicagrelorTicagrelor may increase the anticoagulant activities of Edetic Acid.
TiclopidineTiclopidine may increase the anticoagulant activities of Edetic Acid.
TinzaparinEdetic Acid may increase the anticoagulant activities of Tinzaparin.
TipranavirTipranavir may increase the anticoagulant activities of Edetic Acid.
TirofibanTirofiban may increase the anticoagulant activities of Edetic Acid.
TolmetinTolmetin may increase the anticoagulant activities of Edetic Acid.
TositumomabThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Tositumomab.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Edetic Acid.
VenlafaxineVenlafaxine may increase the anticoagulant activities of Edetic Acid.
VilazodoneVilazodone may increase the anticoagulant activities of Edetic Acid.
Vitamin EVitamin E may increase the anticoagulant activities of Edetic Acid.
VorapaxarThe risk or severity of adverse effects can be increased when Vorapaxar is combined with Edetic Acid.
VortioxetineVortioxetine may increase the anticoagulant activities of Edetic Acid.
WarfarinEdetic Acid may increase the anticoagulant activities of Warfarin.
Food InteractionsNot Available

Targets

1. Lead
Kind
Small molecule
Organism
Human
Pharmacological action
yes
Actions
chelator
References
  1. Onnby L, Giorgi C, Plieva FM, Mattiasson B: Removal of heavy metals from water effluents using supermacroporous metal chelating cryogels. Biotechnol Prog. 2010 Sep-Oct;26(5):1295-302. doi: 10.1002/btpr.422. [PubMed:20945486 ]
  2. Chakraborty N, Banerjee A, Pal R: Accumulation of lead by free and immobilized cyanobacteria with special reference to accumulation factor and recovery. Bioresour Technol. 2011 Mar;102(5):4191-5. doi: 10.1016/j.biortech.2010.12.028. Epub 2010 Dec 13. [PubMed:21195608 ]
  3. Tian SK, Lu LL, Yang XE, Huang HG, Brown P, Labavitch J, Liao HB, He ZL: The impact of EDTA on lead distribution and speciation in the accumulator Sedum alfredii by synchrotron X-ray investigation. Environ Pollut. 2011 Mar;159(3):782-8. doi: 10.1016/j.envpol.2010.11.020. Epub 2010 Dec 18. [PubMed:21168940 ]
2. Iron
Kind
Small molecule
Organism
Human
Pharmacological action
unknown
Actions
chelator
References
  1. Hasegawa H, Rahman IM, Kinoshita S, Maki T, Furusho Y: Separation of dissolved iron from the aqueous system with excess ligand. Chemosphere. 2011 Feb;82(8):1161-7. doi: 10.1016/j.chemosphere.2010.12.048. Epub 2011 Jan 3. [PubMed:21208637 ]
3. Manganese cation
Kind
Small molecule
Organism
Human
Pharmacological action
unknown
Actions
chelator
References
  1. Broncel M, Wagner SC, Paul K, Hackenberger CP, Koksch B: Towards understanding secondary structure transitions: phosphorylation and metal coordination in model peptides. Org Biomol Chem. 2010 Jun 7;8(11):2575-9. doi: 10.1039/c001458c. Epub 2010 Mar 29. [PubMed:20485793 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Zinc ion binding
Specific Function:
Catalyzes the hydrolytic deamination of adenosine and 2-deoxyadenosine. Plays an important role in purine metabolism and in adenosine homeostasis. Modulates signaling by extracellular adenosine, and so contributes indirectly to cellular signaling events. Acts as a positive regulator of T-cell coactivation, by binding DPP4. Its interaction with DPP4 regulates lymphocyte-epithelial cell adhesion.
Gene Name:
ADA
Uniprot ID:
P00813
Molecular Weight:
40764.13 Da
References
  1. Abu-Shady MR, Elshafei AM, el-Beih FM, Mohamed LA: Properties of adenosine deaminase in extracts of Asperigillus terricola. Acta Microbiol Pol. 1994;43(3-4):305-11. [PubMed:7740980 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Bournique B, Petry M, Gousset G: Usefulness of statistic experimental designs in enzymology: example with recombinant hCYP3A4 and 1A2. Anal Biochem. 1999 Dec 1;276(1):18-26. [PubMed:10585740 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Protein homodimerization activity
Specific Function:
Has low activity towards the organophosphate paraxon and aromatic carboxylic acid esters. Rapidly hydrolyzes lactones such as statin prodrugs (e.g. lovastatin). Hydrolyzes aromatic lactones and 5- or 6-member ring lactones with aliphatic substituents but not simple lactones or those with polar substituents.
Gene Name:
PON3
Uniprot ID:
Q15166
Molecular Weight:
39607.185 Da
References
  1. Pla A, Rodrigo L, Hernandez AF, Gil F, Lopez O: Effect of metal ions and calcium on purified PON1 and PON3 from rat liver. Chem Biol Interact. 2007 Apr 5;167(1):63-70. Epub 2007 Jan 16. [PubMed:17292339 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Catalyzes the formation of aromatic C18 estrogens from C19 androgens.
Gene Name:
CYP19A1
Uniprot ID:
P11511
Molecular Weight:
57882.48 Da
References
  1. Moslemi S, Vibet A, Papadopoulos V, Camoin L, Silberzahn P, Gaillard JL: Purification and characterization of equine testicular cytochrome P-450 aromatase: comparison with the human enzyme. Comp Biochem Physiol B Biochem Mol Biol. 1997 Sep;118(1):217-27. [PubMed:9418012 ]
  2. Bellino FL, Holben L: Placental estrogen synthetase (aromatase): evidence for phosphatase-dependent inactivation. Biochem Biophys Res Commun. 1989 Jul 14;162(1):498-504. [PubMed:2546553 ]
  3. Zhang F, Zhou D, Kao YC, Ye J, Chen S: Expression and purification of a recombinant form of human aromatase from Escherichia coli. Biochem Pharmacol. 2002 Nov 1;64(9):1317-24. [PubMed:12392814 ]
  4. Milczarek R, Sokolowska E, Hallmann A, Kaletha K, Klimek J: NADPH- and iron-dependent lipid peroxidation inhibit aromatase activity in human placental microsomes. J Steroid Biochem Mol Biol. 2008 Jun;110(3-5):230-5. doi: 10.1016/j.jsbmb.2007.11.004. Epub 2008 Apr 20. [PubMed:18499441 ]
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Drug created on June 13, 2005 07:24 / Updated on May 02, 2016 13:08