CYP19A1 | CYP11, CYP17, CYP19, CYP20 and CYP21 families | IUPHAR/BPS Guide to PHARMACOLOGY

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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
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
Enzyme Reaction
EC Number:

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

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
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


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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 21/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY,