Publication Date:
1982-03-05
Description:
Norethisterone (17 alpha-ethynyl-19-nortestosterone) is an effective irreversible inhibitor of estrogen synthetase (aromatase), the enzyme responsible for the conversion of androgens to estrogens, even at a 2 X 10(-6) molar concentration. This irreversible inactivation, which is directed toward the active site of aromatase and requires the cofactor-reduced nicotinamide adenine dinucleotide phosphate, is both time- and concentration-dependent. Ethisterone (17 alpha-ethynyltestosterone), in contrast, is not a suicide inhibitor of aromatase even at concentrations of 10(-4) molar.〈br /〉〈span class="detail_caption"〉Notes: 〈/span〉Osawa, Y -- Yarborough, C -- HDO4945/HD/NICHD NIH HHS/ -- New York, N.Y. -- Science. 1982 Mar 5;215(4537):1249-51.〈br /〉〈span class="detail_caption"〉Record origin:〈/span〉 〈a href="http://www.ncbi.nlm.nih.gov/pubmed/7058343" target="_blank"〉PubMed〈/a〉
Keywords:
*Aromatase Inhibitors
;
Binding Sites/drug effects
;
Contraceptives, Oral/*pharmacology
;
Estrogens/*biosynthesis
;
Female
;
Humans
;
Kinetics
;
Microsomes/enzymology
;
Norethindrone/*pharmacology
;
Oxidoreductases/*antagonists & inhibitors
;
Placenta/enzymology
;
Pregnancy
Print ISSN:
0036-8075
Electronic ISSN:
1095-9203
Topics:
Biology
,
Chemistry and Pharmacology
,
Computer Science
,
Medicine
,
Natural Sciences in General
,
Physics
