Journal
ACS CHEMICAL BIOLOGY
Volume 3, Issue 5, Pages 282-286Publisher
AMER CHEMICAL SOC
DOI: 10.1021/cb800056r
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Funding
- NIDDK NIH HHS [R37 DK015556, R01 DK015556, R37 DK015556-37, R37 DK15556] Funding Source: Medline
- NIEHS NIH HHS [F30 ES016484, 1F30 ES016484-01, F30 ES016484-01] Funding Source: Medline
- NIGMS NIH HHS [T32 GM070421, 5 T32 GM070421] Funding Source: Medline
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We report here on the design, synthesis, and evaluation of small molecule inhibitors of the interaction between a steroid receptor coactivator and estrogen receptor alpha. These inhibitors are based upon an amphipathic benzene scaffold whose hydrophobic face mimics the leucine-rich alpha-helical consensus sequence on the steroid receptor coactivators that interacts with a shallow groove on estrogen receptor alpha. 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.
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