Synthesis of Selective Inhibitors of 17beta-Hydroxysteroid Dehydrogenase
Abstract
Estradiol works at the level of the genetic material of the breast epithelial cells to control a wide range of genes that determine how fast the cell will grow. Breast cancer cells often remain sensitive to estradiol subsequent to becoming cancer cells. Type I l7beta- hydroxysteroid dehydrogenase (HSD) is the enzyme responsible for reducing the hormone estrone to estradiol in the epithelial cells of the breast. In many cases of breast cancer, elevated quantities of HSD have been observed associating it with abnormal cell proliferation. It has therefore become our task to try and inbibit HSD's catalytic function. We have discovered that dihydroxynaphthoic acids inhibit dehydrogenase enzymes, and we also know how to design variations among this class of inhibitors. With intentions of finding a new cancer therapeutic, it has been our goal to utilize structure-based drug design and molecular modeling to develop selective inhibitors of human HSD and to test these for activity against human breast cancer cells grown in culture.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jul 01, 2002
- Accession Number
- ADA408149
Entities
People
- David L. Vander Jagt
- Jeremy P. Barlow
Organizations
- University of New Mexico