Abstract
The aromatase and estrone sulfatase enzymes are important sources of biologically active estrogens in postmenopausal women with breast cancer. Promising initial results in the treatment of endocrine-responsive breast cancer have been exhibited by 1α25-dihydroxyvitamin D 3 and the synthetic vitamin D analogues MC903 and EB1089. However, these compounds together with vitamin D 3 and vitamin D 3 sulfate did not inhibit the human placental aromatase enzyme when assayed up to 20 μm. Only vitamin D 3 sulfate and 1α25-dihydroxyvitamin D inhibited the estrone sulfatase activity in human placental microsomes, albeit at high concentration (32 and 37% inhibition, respectively with 50 μm each inhibitor). It is unlikely that inhibition of aromatase or estrone sulfatase enzymes contribute to the inhibitory effect of this group of compounds on breast cancer cells in vivo.
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