Therapeutic Targets Database
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TTD Target ID: TTDS00252

Target Information
NameCytochrome P450 19    
Type of targetSuccessful target    
SynonymsAromatase    
CYPXIX    
Estrogen synthetase    
P-450AROM    
DiseaseBreast cancer
[ICD9: 174, 175   ICD10: C50]
[1][2]
Endometriosis
[ICD9: 617   ICD10: N80]
[3][4]
Estrogen disorders[5][6]
Male infertility
[ICD9: 606   ICD10: N46]
[7][8]
McCune-Albright syndrome[9]
Neurodegenerative diseases
[ICD9: 330-337   ICD10: G30-G32]
[10]
Peripheral precocious puberty
[ICD9: 259.1   ICD10: E22.8, E30.1]
[11]
Drug(s)AminoglutethimideApprovedCushing's syndrome and metastatic breast cancer[12]
AnastrozoleApprovedBreast cancer [9][7]
ExemestaneApprovedHormonally-responsive breast cancer[13]
LetrozoleApprovedHormonally-responsive breast cancer[13]
TestolactoneApprovedAdvanced breast cancer[7][8]
Dextromethorphan+quinidinePhase III completedPainful diabetic neuropathy[14]
BGS649Phase IIObese hypogonadotropic hypogonadism
BioChemical ClassOxidoreductases acting on paired donors    
EC NumberEC 1.14.14.1
PathwayAndrogen and estrogen metabolism
Metabolic pathways
UniProt IDP11511
PDB Structure1TQA; 3EQM; 3S79; 3S7S; 4GL5; 4GL7.    
FunctionCatalyzes the formation of aromatic c18 estrogens from c19 androgens.    
SequenceMVLEMLNPIHYNITSIVPEAMPAATMPVLLLTGLFLLVWNYEGTSSIPGPGYCMGIGPLI SHGRFLWMGIGSACNYYNRVYGEFMRVWISGEETLIISKSSSMFHIMKHNHYSSRFGSKL GLQCIGMHEKGIIFNNNPELWKTTRPFFMKALSGPGLVRMVTVCAESLKTHLDRLEEVTN ESGYVDVLTLLRRVMLDTSNTLFLRIPLDESAIVVKIQGYFDAWQALLIKPDIFFKISWL YKKYEKSVKDLKDAIEVLIAEKRRRISTEEKLEECMDFATELILAEKRGDLTRENVNQCI LEMLIAAPDTMSVSLFFMLFLIAKHPNVEEAIIKEIQTVIGERDIKIDDIQKLKVMENFI YESMRYQPVVDLVMRKALEDDVIDGYPVKKGTNIILNIGRMHRLEFFPKPNEFTLENFAK NVPYRYFQPFGFGPRGCAGKYIAMVMMKAILVTLLRRFHVKTLQGQCVESIQKIHDLSLH PDETKNMLEMIFTPRNSDRCLEH
Related US Patent6,316,431
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorALBANOL A[15]
ALPHA-NAPHTHOFLAVONE[16]
ANDROSTENEDIONE[17]
ANDROSTENEDONE[18]
APIGENIN[16]
Aminoglutethemide[19]
Aminoglutethimide[12]
Anastrozole[9][7]
BIOCHANIN[16]
CGS-18320B[16]
CHRYSIN[16]
COUMATE[20]
DEHYDROLEUCODIN[16]
Dextromethorphan+quinidine[14]
Exemestane[13]
FADROZOLE[21]
FADROZOLE[22]
FADROZOLE HCL[23]
FORMESTANE[24]
GARCINONE D[25]
GOSSYPETIN[26]
ISOLICOFLAVONOL[15]
LIAROZOLE[16]
LIQUIRTIGENIN[26]
LUDARTIN[16]
Letrozole[13]
MDL-18962[27]
MONODICTYOCHROMONE B[28]
MORACHALCONE A[15]
MR-16089[16]
MR-20492[16]
MR-20494[16]
MR-20496[29]
MR-20814[29]
MR-20814[16]
NARINGENIN[16]
NSC-122427[30]
NSC-12999[31]
NSC-131736[31]
NSC-19028[16]
NSC-289311[31]
NSC-356483[31]
NSC-356781[31]
NSC-368272[31]
NSC-368280[31]
NSC-369087[31]
NSC-613604[30]
NSC-625409[31]
NSC-666292[31]
NSC-683634[31]
NSC-75308[31]
NSC-93358[30]
NSC-94258[16]
NSC-94891[30]
Rogletimide[32]
Testolactone[7][8]
VOROZOLE[33]
VOROZOLE[16]
YM-511[34]
broussoflavonol F[15]
docosapentaenoic acid[35]
gamma-mangostin[25]
isogemichalcone C[15]
MultitargetDextromethorphan+quinidine[14]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Prostaglandin J2 metabolites inhibit aromatase activity by redox-sensitive mechanisms: potential implications for breast cancer therapy. Int J Cancer. 2003 Feb 20;103(5):600-5. To Reference
Ref 2J Med Chem. 2001 Mar 1;44(5):672-80.A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase. To Reference
Ref 3Aromatase as a therapeutic target in endometriosis. Trends Endocrinol Metab. 2000 Jan-Feb;11(1):22-7. To Reference
Ref 4Aromatase: a key molecule in the pathophysiology of endometriosis and a therapeutic target. Fertil Steril. 1999 Dec;72(6):961-9. To Reference
Ref 5Use of aromatase inhibitors in precocious puberty. Endocr Relat Cancer. 1999 Jun;6(2):303-6. To Reference
Ref 6Physiological levels of estradiol stimulate plasma high density lipoprotein2 cholesterol levels in normal men. J Clin Endocrinol Metab. 1994 Apr;78(4):855-61. To Reference
Ref 7Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9. To Reference
Ref 8Testosterone versus testosterone and testolactone in treating reproductive and sexual dysfunction in men with epilepsy and hypogonadism. Neurology. 1998 Mar;50(3):782-4. To Reference
Ref 9Effective aromatase inhibition by anastrozole in a patient with gonadotropin-independent precocious puberty in McCune-Albright syndrome. J Pediatr Endocrinol Metab. 2002;15 Suppl 3:945-8. To Reference
Ref 10Brain aromatase is neuroprotective. J Neurobiol. 2001 Jun 15;47(4):318-29. To Reference
Ref 11McCune-Albright syndrome--the German experience. J Pediatr Endocrinol Metab. 2002;15 Suppl 3:897-901. To Reference
Ref 12Aminoglutethimide-induced protein free radical formation on myeloperoxidase: a potential mechanism of agranulocytosis. Chem Res Toxicol. 2007 Jul;20(7):1038-45. Epub 2007 Jun 30. To Reference
Ref 13Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51. To Reference
Ref 14Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. To Reference
Ref 15J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera. To Reference
Ref 16Bioorg Med Chem Lett. 2010 May 15;20(10):3050-64. Epub 2010 Apr 8.Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). To Reference
Ref 17J Med Chem. 1994 Jul 8;37(14):2198-205.Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase. To Reference
Ref 18J Med Chem. 1989 Mar;32(3):651-8.Effects of steroid D-ring modification on suicide inactivation and competitive inhibition of aromatase by analogues of androsta-1,4-diene-3,17-dione. To Reference
Ref 19Aromatase inhibitors and their use in the adjuvant setting. Recent Results Cancer Res. 1998;152:277-84. To Reference
Ref 20J Med Chem. 2010 Mar 11;53(5):2155-70.Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template. To Reference
Ref 21J Med Chem. 2005 Nov 17;48(23):7282-9.Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach. To Reference
Ref 22J. Med. Chem. 53(14):5347-5351 (2010) To Reference
Ref 23Bioorg Med Chem Lett. 2008 Aug 15;18(16):4713-5. Epub 2008 Jul 3.Synthesis of 6- or 4-functionalized indoles via a reductive cyclization approach and evaluation as aromatase inhibitors. To Reference
Ref 24J Nat Prod. 2010 Feb 26;73(2):284-98.The taiwaniaquinoids: a review. To Reference
Ref 25J Nat Prod. 2008 Jul;71(7):1161-6. Epub 2008 Jun 18.Xanthones from the botanical dietary supplement mangosteen (Garcinia mangostana) with aromatase inhibitory activity. To Reference
Ref 26Bioorg Med Chem. 2008 Sep 15;16(18):8466-70. Epub 2008 Aug 19.Screening of herbal constituents for aromatase inhibitory activity. To Reference
Ref 27J Med Chem. 1997 Sep 26;40(20):3263-70.6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase. To Reference
Ref 28J Nat Prod. 2008 Dec 1;71(11):1793-1799. Epub 2008 Oct 21.Monodictyochromes A and B, Dimeric Xanthone Derivatives from the Marine Algicolous Fungus Monodictys putredinis. To Reference
Ref 29Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4.Design and synthesis of a new type of non steroidal human aromatase inhibitors. To Reference
Ref 30Eur J Med Chem. 2009 Oct;44(10):4121-7. Epub 2009 May 19.An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors. To Reference
Ref 31J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors. To Reference
Ref 32J Med Chem. 1987 Sep;30(9):1550-4.Analogues of 3-ethyl-3-(4-pyridyl)piperidine-2,6-dione as selective inhibitors of aromatase: derivatives with variable 1-alkyl and 3-alkyl substituents. To Reference
Ref 33J Med Chem. 2008 Jul 24;51(14):4226-38. Epub 2008 Jul 1.Chiral aromatase and dual aromatase-steroid sulfatase inhibitors from the letrozole template: synthesis, absolute configuration, and in vitro activity. To Reference
Ref 34J Med Chem. 2003 Jul 17;46(15):3193-6.First dual aromatase-steroid sulfatase inhibitors. To Reference
Ref 35J Nat Prod. 2006 Apr;69(4):700-3.Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay. To Reference



 

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