Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00289

Target Information
NameAmine oxidase [flavin-containing] A    
Type of targetSuccessful target    
SynonymsMAO-A    
Monoamine oxidase    
Monoamine oxidase A    
DiseaseDepression
[ICD9: 311   ICD10: F32]
[1]
Mood [affective] disorders[2]
Social phobias
[ICD9: 300.23   ICD10: F40.1]
[3]
Drug(s)ClorgylineApprovedParkinson's disease[4]
IsocarboxazidApprovedDepression[1]
MoclobemideApprovedDepression[3]
TranylcypromineApprovedDepression[5][6]
CHF-3381Phase IINeuropathic pain[7]
BioChemical ClassOxidoreductases acting on the CH-NH2 group of donors    
EC NumberEC 1.4.3.4
PathwayArginine and proline metabolism
Drug metabolism - cytochrome P450
Glycine, serine and threonine metabolism
Histidine metabolism
Metabolic pathways
Phenylalanine metabolism
Tryptophan metabolism
Tyrosine metabolism
UniProt IDP21397
PDB Structure1H8Q; 2BXR; 2BXS; 2Z5X; 2Z5Y.    
FunctionCatalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. Mao-A preferentially oxidizes biogenic amines.    
SequenceMENQEKASIAGHMFDVVVIGGGISGLSAAKLLTEYGVSVLVLEARDRVGGRTYTIRNEHV DYVDVGGAYVGPTQNRILRLSKELGIETYKVNVSERLVQYVKGKTYPFRGAFPPVWNPIA YLDYNNLWRTIDNMGKEIPTDAPWEAQHADKWDKMTMKELIDKICWTKTARRFAYLFVNI NVTSEPHEVSALWFLWYVKQCGGTTRIFSVTNGGQERKFVGGSGQVSERIMDLLGDQVKL NHPVTHVDQSSDNIIIETLNHEHYECKYVINAIPPTLTAKIHFRPELPAERNQLIQRLPM GAVIKCMMYYKEAFWKKKDYCGCMIIEDEDAPISITLDDTKPDGSLPAIMGFILARKADR LAKLHKEIRKKKICELYAKVLGSQEALHPVHYEEKNWCEEQYSGGCYTAYFPPGIMTQYG RVIRQPVGRIFFAGTETATKWSGYMEGAVEAGERAAREVLNGLGKVTEKDIWVQEPESKD VPAVEITHTFWERNLPSVSGLLKIIGFSTSVTALGFVLYKYKLLPRS
Related US Patent6,432,991
6,569,470
6,635,667
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorCGS-19281A[8]
CHF-3381[7]
Clorgyline[4]
DECYL (DIMETHYL)PHOSPHINE OXIDE[9]
Flavin-Adenine Dinucleotide[10]
HARMINE[11]
HYDRAZINECARBOXAMIDE[12]
IPRONIAZIDE[13]
Isocarboxazid[1]
Isopsoralen[2]
MOFEGILINE[14]
Moclobemide[3]
NSC-656158[15]
PIPERINE[11]
PNU-22394[16]
Psoralen[2]
TOLOXATONE[17]
TRACIZOLINE[18]
TRYPTAMINE[16]
TRYPTOLINE[18]
Tranylcypromine[5][6]
beta-methoxyamphetamine[19]
cis-2-phenylcyclopropylamine[20]
ethyl 4- (2-oxo-2H-chromene-3-carboxamido)benzoate[21]
AntagonistMMDA[10]
MultitargetCHF-3381[7]
Tranylcypromine[5][6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1MAOIs in the contemporary treatment of depression. Neuropsychopharmacology. 1995 May;12(3):185-219. To Reference
Ref 2Inhibition of rat brain monoamine oxidase activities by psoralen and isopsoralen: implications for the treatment of affective disorders. Pharmacol Toxicol. 2001 Feb;88(2):75-80. To Reference
Ref 3Efficacy of citalopram and moclobemide in patients with social phobia: some preliminary findings. Hum Psychopharmacol. 2002 Dec;17(8):401-5. To Reference
Ref 4Further investigation into the mechanism of tachykinin NK(2) receptor-triggered serotonin release from guinea-pig proximal colon. J Pharmacol Sci. 2009 May;110(1):122-6. Epub 2009 May 8. To Reference
Ref 5Tramadol and another atypical opioid meperidine have exaggerated serotonin syndrome behavioural effects, but decreased analgesic effects, in genetically deficient serotonin transporter (SERT) mice. Int J Neuropsychopharmacol. 2009 Mar 11:1-11. [Epub ahead of print] To Reference
Ref 6Tranylcypromine: new perspectives on an "old" drug. Eur Arch Psychiatry Clin Neurosci. 2006 Aug;256(5):268-73. To Reference
Ref 7Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 8Bioorg Med Chem Lett. 2004 Feb 23;14(4):1003-5.Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands. To Reference
Ref 9Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 10Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 11Bioorg Med Chem Lett. 2010 Jan 15;20(2):537-40. Epub 2009 Nov 26.Proposed structural basis of interaction of piperine and related compounds with monoamine oxidases. To Reference
Ref 12J Med Chem. 2004 Nov 18;47(24):5860-71.Fluorinated phenylcyclopropylamines. 2. Effects of aromatic ring substitution and of absolute configuration on inhibition of microbial tyramine oxidase. To Reference
Ref 13Bioorg Med Chem. 2010 Feb 15;18(4):1659-64. Epub 2010 Jan 4.Design of novel nicotinamides as potent and selective monoamine oxidase a inhibitors. To Reference
Ref 14J Med Chem. 2008 Dec 25;51(24):8019-26.Structural and mechanistic studies of mofegiline inhibition of recombinant human monoamine oxidase B. To Reference
Ref 15J Med Chem. 2010 Feb 25;53(4):1616-26.Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent. To Reference
Ref 16Bioorg Med Chem Lett. 2004 Feb 23;14(4):999-1002.Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation. To Reference
Ref 17J Nat Prod. 2006 Jun;69(6):945-9.Quercetin as the active principle of Hypericum hircinum exerts a selective inhibitory activity against MAO-A: extraction, biological analysis, and computational study. To Reference
Ref 18Bioorg Med Chem Lett. 2004 Jan 19;14(2):527-9.Binding of an imidazopyridoindole at imidazoline I2 receptors. To Reference
Ref 19Bioorg Med Chem. 2009 Mar 15;17(6):2452-60. Epub 2009 Feb 8.Naphthylisopropylamine and N-benzylamphetamine derivatives as monoamine oxidase inhibitors. To Reference
Ref 20Bioorg Med Chem. 2008 Aug 1;16(15):7148-66. Epub 2008 Jun 28.Fluorinated phenylcyclopropylamines. Part 5: Effects of electron-withdrawing or -donating aryl substituents on the inhibition of monoamine oxidases A and B by 2-aryl-2-fluoro-cyclopropylamines. To Reference
Ref 21J Med Chem. 2009 Apr 9;52(7):1935-42.Synthesis, molecular modeling, and selective inhibitory activity against human monoamine oxidases of 3-carboxamido-7-substituted coumarins. To Reference



 

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