Abstract
We report here on the design, synthesis, and evaluation of small molecule inhibitors of the interaction between a steroid receptor coactivator and estrogen receptor α. These inhibitors are based upon an amphipathic benzene scaffold whose hydrophobic face mimics the leucine-rich α-helical consensus sequence on the steroid receptor coactivators that interacts with a shallow groove on estrogen receptor α. Several of these molecules are among the most potent inhibitors of this interaction described to date and are active at low micromolar concentrations in both in vitro models of estrogen receptor action and in cell-based assays of estrogen receptor-mediated coactivator interaction and transcription.
Original language | English (US) |
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Pages (from-to) | 282-286 |
Number of pages | 5 |
Journal | ACS chemical biology |
Volume | 3 |
Issue number | 5 |
DOIs | |
State | Published - May 16 2008 |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine