Inactivation of aromatase by 4-hydroxy-4-androstene-3,17-dione and 4-acetoxy-4-androstene-3,17-dione and sustained effects |
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Authors: | Angela M.H. Brodie Wesley M. Garrett James R. Hendrickson Chon-Hwa Tsai-Morris Patrick A. Marcotte Cecil H. Robinson |
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Affiliation: | 1. Departments of Pharmacology and Experimental Therapeutics at the University of Maryland School of Medicine, Baltimore, Maryland 21201 USA;2. Departments of Pharmacology and Experimental Therapeutics at The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205 USA |
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Abstract: | 4-Hydroxy-4-androstene-3,17-dione (4-OHA) and 4-acetoxy-4-androstene-3,17-dione (4-AcA), in addition to being competitive inhibitors of aromatase, cause time-dependent, irreversible, loss of enzyme activity in both human placental and rat ovarian microsomes. , treatment of rats with 4-OHA also causes loss of ovarian aromatase activity. To test whether this loss of activity could have significance, rats with hormone-dependent, mammary tumors were treated with 4-OHA on alternate weeks. Tumor regression continued to occur during the weeks without treatment. These findings suggest that inactivation of aromatase is important in the mechanism of action of the compounds . |
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