Target Information

Target General Infomation
Target ID
T13260
Former ID
TTDS00252
Target Name
Cytochrome P450 19
Gene Name
CYP19A1
Synonyms
Aromatase; CYPXIX; Estrogen synthetase; P-450AROM; CYP19A1
Target Type
Successful
Disease Advanced breast cancer [ICD9: 174, 175; ICD10: C50]
Bladder cancer [ICD9: 188; ICD10: C67]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Cushing's disease; Metastatic breast cancer [ICD9: 174, 175, 255.0; ICD10: C50, E24]
Dermatological disease [ICD10: L00-L99]
Endometriosis [ICD9: 617; ICD10: N80]
Hormonally-responsive breast cancer [ICD9: 174, 175; ICD10: C50]
Prostate disease [ICD10: N42.9]
Painful diabetic neuropathy [ICD9: 250.6,338,780; ICD10: E10.4, E11.4, E13.4, G89, R52]
Unspecified [ICD code not available]
Function
Catalyzesthe formation of aromatic C18 estrogens from C19 androgens.
BioChemical Class
Oxidoreductases acting on paired donors
Target Validation
T13260
UniProt ID
P11511
EC Number
EC 1.14.14.1
Sequence
MVLEMLNPIHYNITSIVPEAMPAATMPVLLLTGLFLLVWNYEGTSSIPGPGYCMGIGPLI
SHGRFLWMGIGSACNYYNRVYGEFMRVWISGEETLIISKSSSMFHIMKHNHYSSRFGSKL
GLQCIGMHEKGIIFNNNPELWKTTRPFFMKALSGPGLVRMVTVCAESLKTHLDRLEEVTN
ESGYVDVLTLLRRVMLDTSNTLFLRIPLDESAIVVKIQGYFDAWQALLIKPDIFFKISWL
YKKYEKSVKDLKDAIEVLIAEKRRRISTEEKLEECMDFATELILAEKRGDLTRENVNQCI
LEMLIAAPDTMSVSLFFMLFLIAKHPNVEEAIIKEIQTVIGERDIKIDDIQKLKVMENFI
YESMRYQPVVDLVMRKALEDDVIDGYPVKKGTNIILNIGRMHRLEFFPKPNEFTLENFAK
NVPYRYFQPFGFGPRGCAGKYIAMVMMKAILVTLLRRFHVKTLQGQCVESIQKIHDLSLH
PDETKNMLEMIFTPRNSDRCLEH
Drugs and Mode of Action
Drug(s) Aminoglutethimide Drug Info Approved Cushing's disease; Metastatic breast cancer [535103], [542065]
Anastrozole Drug Info Approved Breast cancer [468200], [536772]
Exemestane Drug Info Approved Hormonally-responsive breast cancer [536361], [542079]
FADROZOLE Drug Info Approved Breast cancer [543063], [544743], [551871]
Letrozole Drug Info Approved Hormonally-responsive breast cancer [468263], [536772]
Testolactone Drug Info Approved Advanced breast cancer [536361], [542325]
Atamestane-plus- Toremifene Drug Info Phase 3 Breast cancer [521531]
LIAROZOLE Drug Info Phase 2/3 Dermatological disease [468265], [521791]
BGS-649 Drug Info Phase 2 Endometriosis [523148]
COUMATE Drug Info Phase 2 Breast cancer [531371]
Dextromethorphan+quinidine Drug Info Phase 2 Painful diabetic neuropathy [536078]
NARINGENIN Drug Info Phase 1 Discovery agent [522980]
FORMESTANE Drug Info Withdrawn from market Breast cancer [544725], [551871]
FINROZOLE Drug Info Discontinued in Phase 2 Prostate disease [546744]
NKS-01 Drug Info Discontinued in Phase 2 Bladder cancer [545382]
VOROZOLE Drug Info Discontinued in Phase 2 Discovery agent [545194]
YM-511 Drug Info Discontinued in Phase 2 Breast cancer [545290]
MINAMESTANE Drug Info Terminated Bladder cancer [545235]
Rogletimide Drug Info Terminated Breast cancer [544813]
Inhibitor (+/-)-7-methoxy-2-(4-methoxyphenyl)chroman-4-one Drug Info [528848]
(+/-)-7-methoxy-2-phenylchroman-4-one Drug Info [529180]
(2S)-5,7,2',4'-tetrahydroxyflavanone Drug Info [526180]
(2S)-abyssinone II Drug Info [526180]
(2S)-euchrenone a7 Drug Info [526180]
1-(1-Benzyl-2-biphenyl-4-yl-ethyl)-1H-imidazole Drug Info [529684]
1-(2-(benzo[b]thiophen-4-yl)ethyl)-1H-imidazole Drug Info [529860]
1-(2-phenoxybenzyl)-1H-imidazole Drug Info [551345]
1-(3-(4-fluorophenyl)propyl)-1H-imidazole Drug Info [530867]
1-(3-Methoxy-naphthalen-2-yl)-1H-imidazole Drug Info [527801]
1-(4-Aminophenyl)-2-(1H-imidazol-1-yl)ethanone Drug Info [551225]
1-(4-Cyanobenzyl)-5-methyl-1H-imidazole Drug Info [529291]
1-(4-nitro-2-phenoxybenzyl)-1H-imidazole Drug Info [551345]
1-(4-Nitro-2-phenylsulfanylbenzyl)-1H-imidazole Drug Info [551345]
1-(7-Methoxy-2-phenyl-chroman-4-yl)-1H-imidazole Drug Info [527222]
1-(9-phenyl-9H-fluoren-9-yl)-1H-1,2,4-triazole Drug Info [529860]
1-(9-Phenyl-9H-fluoren-9-yl)1H-imidazole Drug Info [530867]
1-(9H-fluoren-9-yl)-1H-imidazole Drug Info [529860]
1-(biphenyl-3-ylmethyl)-1H-1,2,4-triazole Drug Info [530712]
1-Bromo-4-imidazol-1-ylmethyl-xanthen-9-one Drug Info [535139]
1-Ethyl-5-(imidazol-1-yl-phenyl-methyl)-1H-indole Drug Info [525448]
1-Imidazol-1-ylmethyl-4-nitro-xanthen-9-one Drug Info [535139]
1-Imidazol-1-ylmethylxanthen-9-one Drug Info [551345]
1-Naphthalen-2-yl-1H-imidazole Drug Info [527801]
1-[(7-Fluoronaphth-2-yl)methyl]-1H-imidazole Drug Info [530867]
10-EPI-8-DEOXY-CUMAMBRIN B Drug Info [530867]
11BETA,13-DIHYDRO-10-EPI-8-DEOXYCUMAM-BRIN B Drug Info [530867]
2,3,4-Trimethoxy-4'-amino-trans-stilbene Drug Info [551225]
2,3,5-Trimethoxy-4'-amino-trans-stilbene Drug Info [551225]
2,3-Dimethoxy-4'-amino-trans-stilbene Drug Info [551225]
2,4-Dimethoxy-3'-amino-trans-stilbene Drug Info [551225]
2,4-Dimethoxy-4'-amino-trans-stilbene Drug Info [551225]
2,5-Dimethoxy-4'-amino-trans-stilbene Drug Info [551225]
2-(1H-Imidazol-1-yl)-1-(4-nitrophenyl)ethanone Drug Info [551225]
2-(3-hydroxyphenyl)-7-methoxychroman-4-one Drug Info [529180]
2-(4-hydroxyphenyl)-7-methoxychroman-4-one Drug Info [529180]
2-Imidazol-1-yl-7-methoxy-3-phenyl-chromen-4-one Drug Info [527565]
2-Imidazol-1-ylmethylxanthen-9-one Drug Info [551345]
2-phenyl-2,3-dihydrobenzo[h]chromen-4-one Drug Info [529180]
2-Phenyl-3-pyridin-4-ylmethylene-chroman-4-one Drug Info [526300]
2-Phenyl-4-[1,2,4]triazol-1-yl-chroman-7-ol Drug Info [527222]
3,4'-(Ethane-1,2-diyl)dibenzenamine Drug Info [551225]
3,4,5-Trimethoxy-3'-amino-trans-stilbene Drug Info [551225]
3,4,5-Trimethoxy-4'-amino-trans-stilbene Drug Info [551225]
3,4-bis(3,4-dimethoxyphenyl)furan-2(5H)-one Drug Info [530867]
3,4-Dimethoxy-4'-amino-trans-stilbene Drug Info [551225]
3,5-Diacetoxy-4'-amino-trans-stilbene Drug Info [551225]
3,5-Diamino-4'-amino-trans-stilbene Drug Info [551225]
3,5-Dihydroxyl-4'-amino-trans-stilbene Drug Info [551225]
3,5-Dimethoxy-4'-amino-trans-stilbene Drug Info [551225]
3-((1H-imidazol-1-yl)methyl)-9H-xanthen-9-one Drug Info [551345]
3-(1-ethyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info [528109]
3-(1-methyl-3,4-dihydronaphthalen-2-yl)-pyridine Drug Info [528109]
3-(2,2-Diphenyl-vinyl)-pyridine Drug Info [527456]
3-(3,4-dihydronaphthalen-2-yl)pyridine Drug Info [528109]
3-(3-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info [528109]
3-(4-Amino-phenyl)-1-methyl-pyrrolidine-2,5-dione Drug Info [533480]
3-(4-Amino-phenyl)-3-butyl-piperidine-2,6-dione Drug Info [533478]
3-(4-Amino-phenyl)-3-ethyl-pyrrolidine-2,5-dione Drug Info [533480]
3-(4-Amino-phenyl)-3-heptyl-piperidine-2,6-dione Drug Info [533478]
3-(4-Amino-phenyl)-3-hexyl-piperidine-2,6-dione Drug Info [533478]
3-(4-Amino-phenyl)-3-methyl-pyrrolidine-2,5-dione Drug Info [533480]
3-(4-Amino-phenyl)-3-pentyl-piperidine-2,6-dione Drug Info [533478]
3-(4-Amino-phenyl)-3-propyl-piperidine-2,6-dione Drug Info [533478]
3-(4-Amino-phenyl)-pyrrolidine-2,5-dione Drug Info [533480]
3-(4-methyl-3,4-dihydronaphthalen-2-yl)pyridine Drug Info [528109]
3-(5-Bromo-6-methoxy-naphthalen-2-yl)-pyridine Drug Info [527801]
3-(5-Chloro-6-methoxy-naphthalen-2-yl)-pyridine Drug Info [527801]
3-(6-Ethoxy-naphthalen-2-yl)-pyridine Drug Info [527801]
3-(6-methoxy-3,4-dihydronaphthalen-2-yl)pyridine Drug Info [528109]
3-(6-methoxynaphthalen-2-yl)pyridine Drug Info [529834]
3-(imidazolylmethyl)-4'-methoxyflavone Drug Info [528327]
3-(imidazolylmethyl)-4'-nitroflavone Drug Info [528327]
3-(imidazolylmethyl)-7-methoxy-4'-nitroflavone Drug Info [528327]
3-(imidazolylmethyl)flavone Drug Info [528327]
3-(naphthalen-2-yl)pyridine Drug Info [529834]
3-Amino-4'-amino-trans-stilbene Drug Info [551225]
3-Fluoren-9-ylidenemethyl-pyridine Drug Info [527456]
3-Fluoro-4'-(pyridin-4-ylmethyl)biphenyl-4-ol Drug Info [531085]
3-Indan-(1E)-ylidenemethyl-pyridine Drug Info [527456]
3-Indan-(1Z)-ylidenemethyl-pyridine Drug Info [527456]
3-Methoxyl-4'-amino-trans-stilbene Drug Info [551225]
3-Nitro-4'-nitro-trans-stilbene Drug Info [551225]
3-[3-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[3-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[3-Phenyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[4-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[4-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[4-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[4-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[4-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[4-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Bromo-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Ethoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Ethoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
3-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
3-[7-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
4'-(Pyridin-4-ylmethyl)biphenyl-3,4-diol Drug Info [531085]
4'-(Pyridin-4-ylmethyl)biphenyl-3-amine Drug Info [531085]
4'-bromo-3-(imidazolylmethyl)-7-methoxyflavone Drug Info [528327]
4'-bromo-3-(imidazolylmethyl)flavone Drug Info [528327]
4'-cyano-3-(imidazolylmethyl)-7-methoxyflavone Drug Info [528327]
4'-cyano-3-(imidazolylmethyl)flavone Drug Info [528327]
4-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info [529860]
4-((1H-imidazol-1-yl)methyl)benzonitrile Drug Info [529291]
4-(1-Imidazol-1-yl-vinyl)-benzonitrile Drug Info [534057]
4-(2,2-Diphenyl-vinyl)-pyridine Drug Info [527456]
4-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Drug Info [529860]
4-(3,4,5-Trimethoxyphenethyl)aniline Drug Info [551225]
4-(3,4-Dimethoxyphenethyl)aniline Drug Info [551225]
4-(3,5-Dimethoxyphenethyl)benzenamine Drug Info [551225]
4-ANDROSTENE-3-17-DIONE Drug Info [551374]
4-Bromo-1-imidazol-1-ylmethyl-xanthen-9-one Drug Info [535139]
4-Fluoren-9-ylidenemethyl-pyridine Drug Info [527456]
4-Imidazol-1-yl-2-phenyl-chroman-7-ol Drug Info [527222]
4-Imidazol-1-ylmethyl-1-nitro-xanthen-9-one Drug Info [535139]
4-Imidazol-1-ylmethyl-1-nitrothioxanthen-9-one Drug Info [551345]
4-Imidazol-1-ylmethyl-2-nitroxanthen-9-one Drug Info [551345]
4-Imidazol-1-ylmethyl-3-nitroxanthen-9-one Drug Info [551345]
4-Imidazol-1-ylmethylthioxanthen-9-one Drug Info [551345]
4-Imidazol-1-ylmethylxanthen-9-one Drug Info [551345]
4-Indan-(1E)-ylidenemethyl-pyridine Drug Info [527456]
4-Indan-(1Z)-ylidenemethyl-pyridine Drug Info [527456]
4-[(3'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info [531085]
4-[(4'-Hydroxybiphenyl-4-yl)methyl]pyridine Drug Info [531085]
4-[5-Bromo-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
4-[5-Chloro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
4-[5-Chloro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
4-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
4-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
4-[5-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
4-[5-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
4-[6-Methoxy-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
4-[6-Methoxy-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
4-[6-Methyl-indan-(1E)-ylidenemethyl]-pyridine Drug Info [527456]
4-[6-Methyl-indan-(1Z)-ylidenemethyl]-pyridine Drug Info [527456]
5-((1H-imidazol-1-yl)methyl)-7,8-dihydroquinoline Drug Info [529860]
5-(2-(1H-imidazol-1-yl)ethyl)quinoline Drug Info [529860]
5-Bromo-8-imidazol-1-ylmethyl-chromen-4-one Drug Info [535139]
5-Indan-(1E)-ylidenemethyl-1H-imidazole Drug Info [527475]
5-Indan-(1Z)-ylidenemethyl-1H-imidazole Drug Info [527475]
5-Pyridin-3-yl-1,3-dihydro-2H-indol-2-one Drug Info [529834]
5-Pyridin-3-yl-2,3-dihydro-1H-inden-1-one Drug Info [529834]
5-[5-Bromo-indan-(1E)-ylidenemethyl]-1H-imidazole Drug Info [527475]
5-[5-Bromo-indan-(1Z)-ylidenemethyl]-1H-imidazole Drug Info [527475]
5-[5-Fluoro-indan-(1E)-ylidenemethyl]-pyrimidine Drug Info [527456]
5-[5-Fluoro-indan-(1Z)-ylidenemethyl]-pyrimidine Drug Info [527456]
5-[5-Methoxy-indan-(1E)-ylidenemethyl]-thiazole Drug Info [527456]
5-[5-Methoxy-indan-(1Z)-ylidenemethyl]-thiazole Drug Info [527456]
6-((1H-imidazol-1-yl)methyl)-2H-chromene-2-thione Drug Info [529860]
6-Imidazol-1-yl-isoquinoline Drug Info [529860]
7,4'-Dihydroxyflavone Drug Info [530867]
7-((1H-imidazol-1-yl)methyl)-2H-chromen-2-one Drug Info [529860]
7-((1H-imidazol-1-yl)methyl)-4H-chromen-4-one Drug Info [529860]
7-((1H-imidazol-1-yl)methyl)isoquinoline Drug Info [529860]
7-(2-(1H-imidazol-1-yl)ethoxy)-2H-chromen-2-one Drug Info [527353]
7-hydroxy-2-(3-hydroxyphenyl)chroman-4-one Drug Info [529180]
7-hydroxy-2-phenylchroman-4-one Drug Info [529180]
7-[1,2,4]Triazol-4-ylmethyl-chromen-4-one Drug Info [535139]
8-Imidazol-1-ylmethyl-5-nitro-chromen-4-one Drug Info [535139]
9-Hydroxy-7,8-benzoflavone Drug Info [530867]
ALBANOL A Drug Info [526180]
ALPHA-NAPHTHOFLAVONE Drug Info [530867]
Aminoglutethemide Drug Info [538153]
Aminoglutethimide Drug Info [536445]
Anastrozole Drug Info [535343], [535547]
ANDROSTENEDIONE Drug Info [533863]
ANDROSTENEDONE Drug Info [533387]
APIGENIN Drug Info [530867]
Benzyl-biphenyl-4-ylmethyl-imidazol-1-yl-amine Drug Info [529684]
BGS-649 Drug Info [549087]
BIOCHANIN Drug Info [530867]
Broussoflavonol F Drug Info [526180]
CGS-18320B Drug Info [530867]
CHRYSIN Drug Info [530867]
COUMATE Drug Info [530712]
DEHYDROLEUCODIN Drug Info [530867]
Dextromethorphan+quinidine Drug Info [536374]
Docosapentaenoic acid Drug Info [528166]
Exemestane Drug Info [535836]
FADROZOLE Drug Info [527856]
FINROZOLE Drug Info [526217], [551871]
FORMESTANE Drug Info [530661]
Gamma-mangostin Drug Info [529538]
GARCINONE D Drug Info [529538]
GOSSYPETIN Drug Info [529679]
Isogemichalcone C Drug Info [526180]
ISOLICOFLAVONOL Drug Info [526180]
Letrozole Drug Info [535836]
LIAROZOLE Drug Info [530867]
LIQUIRTIGENIN Drug Info [529679]
LUDARTIN Drug Info [530867]
MDL-18962 Drug Info [534514]
MINAMESTANE Drug Info [533913], [551871]
MONODICTYOCHROMONE B Drug Info [529759]
MORACHALCONE A Drug Info [526180]
MR-16089 Drug Info [530867]
MR-20492 Drug Info [530867]
MR-20494 Drug Info [530867]
MR-20496 Drug Info [534789]
MR-20814 Drug Info [534789]
N-(2-benzyloxy-4-nitrophenyl)methanesulfonamide Drug Info [528691]
N-(2-hexyloxy-4-nitrophenyl)methanesulfonamide Drug Info [528035]
N-(2-nonyloxy-4-nitrophenyl)methanesulfonamide Drug Info [528035]
N-(2-Propyloxy-4-nitrophenyl)methanesulfonamide Drug Info [528035]
N-[2-(4'-Nitrophenyl)ethyl]-imidazole Drug Info [530867]
NARINGENIN Drug Info [530867]
NKS-01 Drug Info [525727], [551871]
NSC-122427 Drug Info [530190]
NSC-12999 Drug Info [529860]
NSC-131736 Drug Info [529860]
NSC-19028 Drug Info [530867]
NSC-289311 Drug Info [529860]
NSC-356483 Drug Info [529860]
NSC-356781 Drug Info [529860]
NSC-368272 Drug Info [529860]
NSC-368280 Drug Info [529860]
NSC-369087 Drug Info [529860]
NSC-613604 Drug Info [530190]
NSC-625409 Drug Info [529860]
NSC-666292 Drug Info [529860]
NSC-683634 Drug Info [529860]
NSC-75308 Drug Info [529860]
NSC-93358 Drug Info [530190]
NSC-94258 Drug Info [530867]
NSC-94891 Drug Info [530190]
Rogletimide Drug Info [533470]
Testolactone Drug Info [535343], [538089]
VOROZOLE Drug Info [529570]
YM-511 Drug Info [526667]
Modulator Atamestane-plus- Toremifene Drug Info [529105]
Org-33201 Drug Info
Pathways
BioCyc Pathway Superpathway of steroid hormone biosynthesis
Estradiol biosynthesis II
Estradiol biosynthesis I
KEGG Pathway Steroid hormone biosynthesis
Metabolic pathways
Ovarian steroidogenesis
NetPath Pathway FSH Signaling Pathway
PANTHER Pathway Androgen/estrogene/progesterone biosynthesis
PathWhiz Pathway Androgen and Estrogen Metabolism
Reactome Endogenous sterols
WikiPathways Metapathway biotransformation
Tryptophan metabolism
Oxidation by Cytochrome P450
Ovarian Infertility Genes
Metabolism of steroid hormones and vitamin D
FSH signaling pathway
Integrated Breast Cancer Pathway
Phase 1 - Functionalization of compounds
References
Ref 468200(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5137).
Ref 468263(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5209).
Ref 468265(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5210).
Ref 521531ClinicalTrials.gov (NCT00044291) Phase III Study of Atamestane Plus Toremifene Versus Letrozole in Advanced Breast Cancer. U.S. National Institutes of Health.
Ref 521791ClinicalTrials.gov (NCT00282724) Efficacy and Safety of Two Doses of Liarozole vs. Placebo for the Treatment of Lamellar Ichthyosis. U.S. National Institutes of Health.
Ref 522980ClinicalTrials.gov (NCT01091077) A Pilot Study of the Grapefruit Flavonoid Naringenin for HCV Infection. U.S. National Institutes of Health.
Ref 523148ClinicalTrials.gov (NCT01190475) BGS649 Monotherapy in Moderate to Severe Endometriosis Patients. U.S. National Institutes of Health.
Ref 531371Irosustat: a first-generation steroid sulfatase inhibitor in breast cancer. Expert Rev Anticancer Ther. 2011 Feb;11(2):179-83.
Ref 535103Breakdown of Th cell immune responses and steroidogenic CYP11A1 expression in CD4+ T cells in a murine model implanted with B16 melanoma. Cell Immunol. 2000 Nov 25;206(1):7-15.
Ref 536078Dextromethorphan/quinidine: AVP 923, dextromethorphan/cytochrome P450-2D6 inhibitor, quinidine/dextromethorphan. Drugs R D. 2005;6(3):174-7.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536772New drugs in development for the treatment of endometriosis. Expert Opin Investig Drugs. 2008 Aug;17(8):1187-202.
Ref 542065(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7054).
Ref 542079(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7073).
Ref 542325(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7303).
Ref 543063(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8311).
Ref 544725Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000733)
Ref 544743Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000824)
Ref 544813Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001207)
Ref 545194Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002428)
Ref 545235Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002545)
Ref 545290Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002721)
Ref 545382Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003076)
Ref 546744Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010074)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 525448Bioorg Med Chem Lett. 1999 Feb 8;9(3):333-6.New selective nonsteroidal aromatase inhibitors: synthesis and inhibitory activity of 2,3 or 5-(alpha-azolylbenzyl)-1H-indoles.
Ref 525727Effects of aromatase inhibitors on the pathobiology of the human breast, endometrial and ovarian carcinoma. Endocr Relat Cancer. 1999 Jun;6(2):197-204.
Ref 526180J Nat Prod. 2001 Oct;64(10):1286-93.Aromatase inhibitors from Broussonetia papyrifera.
Ref 526217Pharmacokinetics of finrozole (MPV-2213ad), a novel selective aromatase inhibitor, in healthy men. Br J Clin Pharmacol. 2001 Dec;52(6):702-4.
Ref 526300Bioorg Med Chem Lett. 2002 Apr 8;12(7):1059-61.New aromatase inhibitors. Synthesis and inhibitory activity of pyridinyl-substituted flavanone derivatives.
Ref 526667J Med Chem. 2003 Jul 17;46(15):3193-6.First dual aromatase-steroid sulfatase inhibitors.
Ref 527222Bioorg Med Chem Lett. 2004 Oct 18;14(20):5215-8.Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Ref 527353J Med Chem. 2004 Dec 30;47(27):6792-803.Design, synthesis, and 3D QSAR of novel potent and selective aromatase inhibitors.
Ref 527456J Med Chem. 2005 Mar 10;48(5):1563-75.Synthesis and evaluation of (pyridylmethylene)tetrahydronaphthalenes/-indanes and structurally modified derivatives: potent and selective inhibitors of aldosterone synthase.
Ref 527475J Med Chem. 2005 Mar 24;48(6):1796-805.Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imidazolylmethyleneindanes: potent inhibitors of aldosterone synthase.
Ref 527565Bioorg Med Chem. 2005 Jun 2;13(12):4063-70. Epub 2005 Apr 25.Synthesis and characterization of azole isoflavone inhibitors of aromatase.
Ref 527801J Med Chem. 2005 Oct 20;48(21):6632-42.Heteroaryl-substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis.
Ref 527856J Med Chem. 2005 Nov 17;48(23):7282-9.Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.
Ref 528035J Med Chem. 2006 Feb 23;49(4):1413-9.Novel sulfonanilide analogues suppress aromatase expression and activity in breast cancer cells independent of COX-2 inhibition.
Ref 528109J Med Chem. 2006 Apr 6;49(7):2222-31.Synthesis and evaluation of heteroaryl-substituted dihydronaphthalenes and indenes: potent and selective inhibitors of aldosterone synthase (CYP11B2) for the treatment of congestive heart failure and myocardial fibrosis.
Ref 528166J Nat Prod. 2006 Apr;69(4):700-3.Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.
Ref 528327J Med Chem. 2006 Jul 27;49(15):4777-80.Lead optimization providing a series of flavone derivatives as potent nonsteroidal inhibitors of the cytochrome P450 aromatase enzyme.
Ref 528691J Med Chem. 2007 Apr 5;50(7):1635-44. Epub 2007 Feb 22.Synthesis and biological evaluation of selective aromatase expression regulators in breast cancer cells.
Ref 528848J Med Chem. 2007 Jun 14;50(12):2799-806. Epub 2007 May 19.Synthesis and biological evaluation of (+/-)-abyssinone II and its analogues as aromatase inhibitors for chemoprevention of breast cancer.
Ref 529105J Steroid Biochem Mol Biol. 2008 Jan;108(1-2):1-7. Epub 2007 Sep 7.Toremifene-atamestane; alone or in combination: predictions from the preclinical intratumoral aromatase model.
Ref 529180Bioorg Med Chem. 2008 Feb 1;16(3):1474-80. Epub 2007 Oct 22.New 7,8-benzoflavanones as potent aromatase inhibitors: synthesis and biological evaluation.
Ref 529291J Med Chem. 1991 Feb;34(2):725-36.Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.
Ref 529538J 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.
Ref 529570J 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.
Ref 529679Bioorg Med Chem. 2008 Sep 15;16(18):8466-70. Epub 2008 Aug 19.Screening of herbal constituents for aromatase inhibitory activity.
Ref 529684Bioorg Med Chem. 2008 Sep 15;16(18):8349-58. Epub 2008 Aug 26.CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.
Ref 529759J 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.
Ref 529834J Med Chem. 2008 Dec 25;51(24):8077-87.In vivo active aldosterone synthase inhibitors with improved selectivity: lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivatives.
Ref 529860J Med Chem. 2009 Jan 8;52(1):143-50.Fast three dimensional pharmacophore virtual screening of new potent non-steroid aromatase inhibitors.
Ref 530190Eur J Med Chem. 2009 Oct;44(10):4121-7. Epub 2009 May 19.An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors.
Ref 530661J Nat Prod. 2010 Feb 26;73(2):284-98.The taiwaniaquinoids: a review.
Ref 530712J Med Chem. 2010 Mar 11;53(5):2155-70.Highly potent first examples of dual aromatase-steroid sulfatase inhibitors based on a biphenyl template.
Ref 530867Bioorg 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).
Ref 531085J Med Chem. 2010 Aug 12;53(15):5749-58.Replacement of imidazolyl by pyridyl in biphenylmethylenes results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for the treatment of prostate cancer.
Ref 533387J 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.
Ref 533470J 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.
Ref 533478J Med Chem. 1986 Aug;29(8):1362-9.Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones.
Ref 533480J Med Chem. 1986 Apr;29(4):520-3.Synthesis and biochemical evaluation of analogues of aminoglutethimide based on phenylpyrrolidine-2,5-dione.
Ref 533863J 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.
Ref 533913High-performance liquid chromatographic determination of FCE 24928, a new aromatase inhibitor, in human plasma. J Chromatogr A. 1994 Feb 4;660(1-2):293-8.
Ref 534057J Med Chem. 1993 May 14;36(10):1393-400.Aromatase inhibitors: synthesis, biological activity, and binding mode of azole-type compounds.
Ref 534514J Med Chem. 1997 Sep 26;40(20):3263-70.6 beta-Propynyl-substituted steroids: mechanism-based enzyme-activated irreversible inhibitors of aromatase.
Ref 534789Bioorg Med Chem Lett. 1998 May 5;8(9):1041-4.Design and synthesis of a new type of non steroidal human aromatase inhibitors.
Ref 535139A 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. J Med Chem. 2001 Mar 1;44(5):672-80.
Ref 535343Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9.
Ref 535547Effective 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.
Ref 535836Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51.
Ref 536374Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.
Ref 536445Aminoglutethimide-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.
Ref 538089Testosterone versus testosterone and testolactone in treating reproductive and sexual dysfunction in men with epilepsy and hypogonadism. Neurology. 1998 Mar;50(3):782-4.
Ref 538153Aromatase inhibitors and their use in the adjuvant setting. Recent Results Cancer Res. 1998;152:277-84.
Ref 549087Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800032111)
Ref 551225Design, synthesis, and biological evaluation of resveratrol analogues as aromatase and quinone reductase 2 inhibitors for chemoprevention of cancer. Bioorg Med Chem. 2010 Jul 15;18(14):5352-66. doi: 10.1016/j.bmc.2010.05.042. Epub 2010 May 24.
Ref 551345Novel highly potent and selective nonsteroidal aromatase inhibitors: synthesis, biological evaluation and structure-activity relationships investigation. J Med Chem. 2010 Jul 22;53(14):5347-51. doi: 10.1021/jm100319h.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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