PMID: 6540337Jun 1, 1984Paper

Time-dependent inhibition of aromatase in trophoblastic tumor cells in tissue culture

Journal of Steroid Biochemistry
J O JohnstonB W Metcalf

Abstract

Human choriocarcinoma trophoblast cells (JAr line) were utilized as whole cell preparations in tissue culture to evaluate the effects of mechanism-based inactivation or "suicide inhibition" of estrogen biosynthesis. A C-19 acetylenic analog (MDL 18,962) of the substrate, androstenedione, was evaluated in competitive and time-dependent assays. Product formation was determined by accumulation of 3H2O resulting from the stereo-specific elimination of 1 beta-tritium from the androgen substrate. Trophoblast cells exhibited initial linear kinetics for at least 3 h following addition of [1-3H]androstenedione. The Km for androstenedione was 35.1 nM with Vmax of 3.7 pmol/h/10(6) trophoblast cells. Kinetic analysis of time-dependent inhibition of aromatase in trophoblast cells revealed an apparent Ki of 0.6 nM for MDL 18,962 and at t 1/2 of inactivation of 26 min at infinite inhibitor concentration. These studies suggest that a suicide aromatase inhibitor can cause irreversible inhibition of estrogen biosynthesis in intact trophoblast cells. In the presence of 1 nM or 10 nM MDL 18,962, trophoblast cells exhibited initial linear kinetics for estrogen biosynthesis during the first hour following co-incubation with inhibitor and 33 nM subst...Continue Reading

References

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Citations

Jan 1, 1994·Breast Cancer Research and Treatment·R W Brueggemeier
Nov 1, 1986·Journal of Steroid Biochemistry·D HendersonM F el Etreby
Jan 1, 1987·Journal of Steroid Biochemistry·D Henderson
Oct 1, 1989·Journal of Steroid Biochemistry·J O JohnstonR C Shumaker
Jul 1, 1987·Steroids·G D BerkovitzM Fujimoto
Nov 20, 1990·The Journal of Steroid Biochemistry and Molecular Biology·R W BrueggemeierN E Katlic
Apr 1, 1991·The Journal of Steroid Biochemistry and Molecular Biology·M D KrekelsP A Janssen
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Aug 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·D ZhouS Chen
Jan 1, 1995·The Journal of Steroid Biochemistry and Molecular Biology·J O JohnstonG W Holbert
Apr 1, 1997·The Journal of Steroid Biochemistry and Molecular Biology·R W BrueggemeierC J Lovely
Aug 21, 2002·Breast Cancer Research and Treatment·Robert W Brueggemeier
Sep 11, 2001·American Journal of Therapeutics·R W Brueggemeier
Mar 1, 1985·Steroids·J P BurkhartJ O Johnston
Jan 1, 1990·Journal of Enzyme Inhibition·R W Brueggemeier
Apr 9, 2005·Endocrine Reviews·Robert W BrueggemeierEdgar S Diaz-Cruz
Jan 1, 1988·Journal of Enzyme Inhibition·R B Silverman

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