Citation

Numazawa M, Mutsumi A, Hoshi K, Tanaka Y. Biochem. Biophys. Res. Commun. 1992; 186(1): 32-39.

Copyright

(Copyright © 1992, Academic Press)

DOI

10.1016/s0006-291x(05)80771-5

PMID

1632774

Abstract

5-En-7-one steroid 1 was found to be a potent inhibitor of aromatase. This along with its 19-hydroxy derivative 7 was characterized as suicide substrate of human placental aromatase (k(inact)'s of 0.069 and 0.058 min-1 and KI's of 143 nM and 11.1 microM, respectively, for steroids 1 and 7). The results suggest that the 19-oxygenation would be involved in the irreversible inactivation of aromatase by the 5-en-7-one steroids.

Language: en

Keywords

Androstenedione; Aromatase; Aromatase Inhibitors; Binding, Competitive; Female; Humans; Indicators and Reagents; Kinetics; Magnetic Resonance Spectroscopy; Microsomes; Molecular Structure; Placenta; Pregnancy; Substrate Specificity