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MRC Group in Molecular Endocrinology, CHUL Research Center, and Laval University, Quebec, GIV 4G2, Canada
Estrogens are well known to play a predominant role in human breast cancer. The current endocrine therapy of breast cancer consists in administering an antiestrogen which blocks the action of estrogens at the receptor level. However, the currently available antiestrogens possess mixed estrogenic and antiestrogenic activity, thus limiting their potential therapeutic efficacy. The present data show that a series of new estrogen derivatives demonstrate not only pure antiestrogenic activity in the sensitive in vivo mouse uterus assay, but simultaneously exert potent inhibitory effects on 17ß-hydroxysteroid dehydrogenase activity, the enzyme responsible for the formation of 17ß-estradiol from estrone, the last step in estrogen formation. Such compounds having a dual site of inhibitory action, namely on estrogen formation and on the estrogen receptor, could well lead to an improved endocrine therapy of breast and other estrogen-sensitive cancers as well as other nonmalignant estrogen-sensitive diseases.
1 Holder of a postdoctoral fellowship from MRC Canada.
2 Holder of a Studentship from Fonds de la Recherche en Santé du Québec.
3 To whom requests for reprints should be addressed, at Laboratory of Molecular Endocrinology, CHUL Research Center, 2705 Laurier Boulevard, Quebec, QC, G1V 4G2, Canada.
Received 7/15/91. Accepted 11/11/91.
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