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Endocrinology, Vol 108, 1597-1599, Copyright © 1981 by Endocrine Society

ARTICLES

Enzyme-generated intermediates derived from 4-androstene-3,6,17-trione and 1,4,6-androstatriene-3,17-dione cause a time-dependent decrease in human placental aromatase activity

DF Covey and WF Hood

Kinetic evidence is presented for a time-dependent decrease in human placental aromatase activity by enzyme-generated intermediates derived from two widely used steroids previously described as competitive inhibitors of estrogen biosynthesis. Thus, 4-androstene-3,6,17-trione binds to the enzyme with an apparent Ki of 0.43 microM and has a pseudo- first order overall rate constant for decrease in activity of 4.03x10(- 3)sec-1, while 1,4,6-androstatriene-3,17-dione has an apparent Ki of 0.18 microM and a pseudo-first order overall rate constant for decrease in activity of 1.10x10(-3)sec-1. These findings imply that the potent inhibition of estrogen biosynthesis caused by these steroids results primarily from a decrease in enzyme activity caused by enzyme-generated intermediates from the parent steroids.


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