14.ALPHA.-Hydroxyandrost-4-ene-3,6,17-trione as a mechanical-based irreversible inhibitor of estrogen biosynthesis.
Year: 1990
Type: article
Abstract: Various derivatives of androst-4-ene-3,17-dione derived from microbial transformation were evaluated as inhibitors of human placental aromatase. 14 alpha-Hydroxyandrost-4-ene-3,6,17-trione was the most potent inhibitor showing a time-dependent, pseudo-first-order inactivation of aromatase in the presence of reduced nicotinamide adenine dinucleotide phosphate with apparent Ki of 1.3 microM and Kinact of 0.23 min-1. This compound also inhibited aromatase in rat ovary and suppressed serum estradiol levels in in vivo experiments.
DOI: 10.1248/cpb.38.2834
Authors: Makoto YOSHIHAMA, Kohji TAMURA, Masamichi NAKAKOSHI, Junji NAKAMURA, Nobuaki FUJISE, Gosei KAWANISHI
Institution: Megmilk Snow Brand (Japan)
Language: English
Subfield: Endocrinology
Domain: Life Sciences
Open Access status: bronze
OpenAlex ID: W2003148204