A high-throughput screen to identify inhibitors of aromatase (CYP19)

Analytical Biochemistry

Volumn 284, Issue 2, 2000, Pages 427-430

  Stresser, David M ^a   Turner, Stephanie D ^a   McNamara, Joanne ^a   Stocker, Penny ^a   Miller, Vaughn P ^a   Crespi, Charles L ^a   Patten, Christopher J ^a  

^a Gentest Corporation   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BIOCHEMISTRY;

AROMATASE; HIGH-THROUGHPUT SCREENS;

CHEMISTRY;

19 ETHYLDITHIOANDROSTENEDIONE; 19 ETHYLTHIO 4 ENE 3,17 DIONE; 19 MERCAPTOANDRO 4 ENE 3,17 DIONE; ANDROGEN; ANDROSTENEDIONE; ANDROSTENEDIONE DERIVATIVE; AROMATASE; AROMATASE INHIBITOR; CHRYSIN; ESTRADIOL; ESTROGEN; ESTRONE; FLAVONOID; FURAFYLLINE; KETOCONAZOLE; NARINGENIN; ORG 30365; QUERCETIN; QUINIDINE; STEROID; SULFAPHENAZOLE; TESTOSTERONE; TRANYLCYPROMINE; UNCLASSIFIED DRUG;

ANDROGEN METABOLISM; ANIMAL CELL; AROMATIZATION; ARTICLE; CELL CULTURE; DRUG SCREENING; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME SUBSTRATE; FLUOROMETRY; HUMAN; HUMAN CELL; HUMAN TISSUE; ISOTOPE LABELING; NONHUMAN; PLACENTA; PRIORITY JOURNAL; XENOBIOTIC METABOLISM;

EID: 0034633287     PISSN: 00032697     EISSN: None     Source Type: Journal    
DOI: 10.1006/abio.2000.4729     Document Type: Article

References (20)

1. The involvement of human placental microsomal cytochrome P-450 in aromatization
2. Diverse functions of aromatase: O-deethylation of 7-ethoxycoumarin
3. Aromatase and its inhibitors
4. A yeast screen system for aromatase inhibitors and ligands for androgen receptor: Yeast cells transformed with aromatase and androgen receptor
5. Assay of aromatase activity
6. Stable expression of human aromatase complementary DNA in mammalian cells: A useful system for aromatase inhibitor screening
7. Fast liquid chromatographic assay of androgen aromatase activity
8. Rapid assay of aromatase activity by fast liquid chromatography: Spectroscopic evaluation of metabolite profiles indicate unexpected pitfalls
9. Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes P450
10. CYP19 (Aromatase): Characterization of the recombinant enzyme and its role in the biotransformation of xenobiotics
11. Inactivation of aromatase in vitro by 4-hydroxy-4-androstene-3,17-dione and 4-acetoxy-4-androstene-3,17-dione and sustained effects in vivo
12. Selection of 19-(ethyl-dithio)-androst-4-ene-3,17-dione (ORG 30958): A potent aromatase inhibitor in vivo
13. Reversible inhibition of human placental microsomal aromatase by CGS 18320B and other non-steroidal compounds
14. Inhibition of human estrogen synthetase (aromatase) by flavones
15. Structure-activity relationships of the inhibition of human placental aromatase by imidazole drugs including ketoconazole
16. Expression of xenobiotic-metabolizing cytochrome P450 forms in human full-term placenta
17. Molecular basis of the inhibition of human aromatase (estrogen synthetase) by flavone and isoflavone phytoestrogens: A site-directed mutagenesis study
18. Flavonoid inhibition of aromatase enzyme activity in human preadipocytes
19. Ovine placental aromatase: Studies of activity levels, kinetic characteristics and effects of aromatase inhibitors
20. Screening of potential cancer preventing chemicals as aromatase inhibitors in an in vitro assay