Development of peptide antagonists that target estrogen receptor-cofactor interactions.
Publication
, Journal Article
McDonnell, DP; Chang, CY; Norris, JD
Published in: J Steroid Biochem Mol Biol
November 30, 2000
We have developed a series of high-affinity peptide antagonists that inhibit the transcriptional activity of both subtypes of the human estrogen receptor (ERalpha and ERbeta). We believe that it will be possible to develop these peptides, or corresponding peptidomimetic derivatives, into pharmaceuticals for use in the treatment of breast cancer and other estrogenopathies. It is anticipated that drugs of this type could be used in combination with classical antiestrogens, such as tamoxifen, to achieve a complete blockage of ER-transcriptional activity. Although ER has been the primary target of our studies to date, it is likely that the insights gained from this work will apply to other nuclear receptors and transcription factors.
Duke Scholars
Published In
J Steroid Biochem Mol Biol
DOI
ISSN
0960-0760
Publication Date
November 30, 2000
Volume
74
Issue
5
Start / End Page
327 / 335
Location
England
Related Subject Headings
- Transcriptional Activation
- Transcription Factors
- Tamoxifen
- Substrate Specificity
- Receptors, Estrogen
- Protein Binding
- Peptides
- Molecular Sequence Data
- Humans
- Estrogen Receptor Modulators
Citation
APA
Chicago
ICMJE
MLA
NLM
McDonnell, D. P., Chang, C. Y., & Norris, J. D. (2000). Development of peptide antagonists that target estrogen receptor-cofactor interactions. J Steroid Biochem Mol Biol, 74(5), 327–335. https://doi.org/10.1016/s0960-0760(00)00109-6
McDonnell, D. P., C. Y. Chang, and J. D. Norris. “Development of peptide antagonists that target estrogen receptor-cofactor interactions.” J Steroid Biochem Mol Biol 74, no. 5 (November 30, 2000): 327–35. https://doi.org/10.1016/s0960-0760(00)00109-6.
McDonnell DP, Chang CY, Norris JD. Development of peptide antagonists that target estrogen receptor-cofactor interactions. J Steroid Biochem Mol Biol. 2000 Nov 30;74(5):327–35.
McDonnell, D. P., et al. “Development of peptide antagonists that target estrogen receptor-cofactor interactions.” J Steroid Biochem Mol Biol, vol. 74, no. 5, Nov. 2000, pp. 327–35. Pubmed, doi:10.1016/s0960-0760(00)00109-6.
McDonnell DP, Chang CY, Norris JD. Development of peptide antagonists that target estrogen receptor-cofactor interactions. J Steroid Biochem Mol Biol. 2000 Nov 30;74(5):327–335.
Published In
J Steroid Biochem Mol Biol
DOI
ISSN
0960-0760
Publication Date
November 30, 2000
Volume
74
Issue
5
Start / End Page
327 / 335
Location
England
Related Subject Headings
- Transcriptional Activation
- Transcription Factors
- Tamoxifen
- Substrate Specificity
- Receptors, Estrogen
- Protein Binding
- Peptides
- Molecular Sequence Data
- Humans
- Estrogen Receptor Modulators