CYP19A1

Target id: 1362

Nomenclature: CYP19A1

Abbreviated Name: Aromatase

Family: CYP11, CYP17, CYP19, CYP20 and CYP21 families

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for CYP19A1 in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 503 15q21 CYP19A1 cytochrome P450 family 19 subfamily A member 1
Mouse - 503 9 29.49 cM Cyp19a1 cytochrome P450, family 19, subfamily a, polypeptide 1
Rat - 508 8q23-q24 Cyp19a1 cytochrome P450, family 19, subfamily a, polypeptide 1
Previous and Unofficial Names
ARO | ARO1 | Cytochrome P450 19 aromatase | cytochrome P450 19A1 | cytochrome P450, family 19, subfamily a, polypeptide 1 | estrogen synthase | ArKO | cytochrome P450, family 19, subfamily A, polypeptide 1 | cytochrome P450
Database Links
BRENDA
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
SynPHARM
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 1.14.14.1

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
letrozole Hs Inhibition 10.7 pKi 4
pKi 10.7 (Ki 2x10-11 M) [4]
azalanstat Hs Inhibition 8.1 pKi 7
pKi 8.1 (Ki 7.6x10-9 M) [7]
testolactone Hs Inhibition 4.5 pKi 3
pKi 4.5 (Ki 3.5x10-5 M) [3]
fadrozole Hs Inhibition 8.4 pIC50 1
pIC50 8.4 (IC50 4.5x10-9 M) [1]
anastrozole Hs Inhibition 7.8 pIC50 5
pIC50 7.8 (IC50 1.5x10-8 M) [5]
exemestane Hs Inhibition 7.3 pIC50 2
pIC50 7.3 (IC50 5.01x10-8 M) [2]
Description: Inhibition of aromatase (CYP19A1) extracted to homogeneity from human placenta.
aminoglutethimide Hs Inhibition - - 6
[6]
Inhibitor Comments
The reference for aminoglutethimide presents graphical data confirming the inhibition of CYP19A1 by this drug, but does present calculated Ki values [6].
Clinically-Relevant Mutations and Pathophysiology
Disease:  Aromatase deficiency
OMIM: 613546
Orphanet: ORPHA91
Disease:  Aromatase excess syndrome
OMIM: 139300
Orphanet: ORPHA178345

References

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1. Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A. (1991) Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J. Med. Chem.34 (2): 725-36. [PMID:1825337]

2. Christiansen JS. (1985) Glomerular hyperfiltration in diabetes mellitus. Diabet. Med.2 (4): 235-9. [PMID:2951074]

3. Covey DF, Hood WF. (1982) A new hypothesis based on suicide substrate inhibitor studies for the mechanism of action of aromatase. Cancer Res.42 (8 Suppl): 3327s-3333s. [PMID:7083195]

4. Mayhoub AS, Marler L, Kondratyuk TP, Park EJ, Pezzuto JM, Cushman M. (2012) Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrol. Bioorg. Med. Chem.20 (7): 2427-34. [PMID:22386564]

5. Muftuoglu Y, Mustata G. (2010) Pharmacophore modeling strategies for the development of novel nonsteroidal inhibitors of human aromatase (CYP19). Bioorg. Med. Chem. Lett.20 (10): 3050-64. [PMID:20413308]

6. Payne EJ, Ingley E, Dick IM, Wilson SG, Bond CS, Prince RL. (2009) In vitro kinetic properties of the Thr201Met variant of human aromatase gene CYP19A1: functional responses to substrate and product inhibition and enzyme inhibitors. J. Clin. Endocrinol. Metab.94 (8): 2998-3002. [PMID:19470632]

7. Walker KA, Kertesz DJ, Rotstein DM, Swinney DC, Berry PW, So OY, Webb AS, Watson DM, Mak AY, Burton PM et al.. (1993) Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering. J. Med. Chem.36 (15): 2235-7. [PMID:8340925]

How to cite this page

CYP11, CYP17, CYP19, CYP20 and CYP21 families: CYP19A1. Last modified on 18/09/2015. Accessed on 18/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1362.