CHED 816 |
| Ruth E. Bringman, Smita S. Muddana, and Blake R. Peterson. Department of Chemistry, The Pennsylvania State University, 152 Davey Lab, University Park, PA 16802 |
| Estrogen receptors (ERs) are ligand-regulated transcriptional factors that play key roles in the progression of numerous diseases including breast cancer. Small-molecule antiestrogens such as tamoxifen and ICI 164,384 are clinically employed for the treatment of diseases dependent on estrogens. These compounds function as antiestrogens that block ER-mediated gene expression by binding tightly to ERs and projecting hydrophobic side-chains that disrupt interactions between estrogen receptors and transcriptional coactivator proteins. We are investigating structurally related ER ligands as antiestrogens and tools for probing ER function. These compounds include metabolically stable oxime derivatives of estrone that comprise potent ER ligands in whole cell assays. We will report efforts to identify estrone oximes linked to hydrophobic side chains as potential antiestrogens effective against breast cancer cells. |
|
Undergraduate Research Poster Session: Organic Chemistry
2:00 PM-4:00 PM, Monday, March 29, 2004 Anaheim Convention Center -- Hall A, Poster
Division of Chemical Education |
