Peptide antagonists of the human estrogen receptor.
Estrogen receptor alpha transcriptional activity is regulated by distinct conformational states that are the result of ligand binding. Phage display was used to identify peptides that interact specifically with either estradiol- or tamoxifen-activated estrogen receptor alpha. When these peptides were coexpressed with estrogen receptor alpha in cells, they functioned as ligand-specific antagonists, indicating that estradiol-agonist and tamoxifen-partial agonist activities do not occur by the same mechanism. The ability to regulate estrogen receptor alpha transcriptional activity by targeting sites outside of the ligand-binding pocket has implications for the development of estrogen receptor alpha antagonists for the treatment of tamoxifen-refractory breast cancers.
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Related Subject Headings
- Transcription, Genetic
- Transcription Factor AP-1
- Tamoxifen
- Recombinant Fusion Proteins
- Receptors, Estrogen
- Receptors, Cytoplasmic and Nuclear
- Peptides
- Peptide Library
- Molecular Sequence Data
- Mifepristone
Citation
Published In
DOI
ISSN
Publication Date
Volume
Issue
Start / End Page
Location
Related Subject Headings
- Transcription, Genetic
- Transcription Factor AP-1
- Tamoxifen
- Recombinant Fusion Proteins
- Receptors, Estrogen
- Receptors, Cytoplasmic and Nuclear
- Peptides
- Peptide Library
- Molecular Sequence Data
- Mifepristone