Role of Sulfation Pharmacogenetics in Breast Cancer Treatment with 2-Methoxyestradiol
Final rept. 1 Oct 2000-30 Sep 2001
MAYO FOUNDATION ROCHESTER MN
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2-ME2 is an endogenous estrogen metabolite that inhibits the proliferation of breast and other human cancer cell lines. 2-ME2 also has potent anti-angiogenic and anti-tubulin properties, and it may inhibit estrogen- induced carcinogenesis in the mammary gland. We set out to test the hypothesis that 2-ME2 might be a substrate for sulfate conjugation and, therefore, that individual variations in the sulfation of 2-ME2 might contribute to individual differences in its metabolism, pharmacokinetics and therapeutic efficacy. As a first step, we tested 2-ME2 as a substrate for 7 human sulfotransferase SULT isoforms -- as well as all of the common allozymes for SULT 1 Al and 1A2.
- Medicine and Medical Research