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Peptide antagonists of the human estrogen receptor.

Publication ,  Journal Article
Norris, JD; Paige, LA; Christensen, DJ; Chang, CY; Huacani, MR; Fan, D; Hamilton, PT; Fowlkes, DM; McDonnell, DP
Published in: Science
July 30, 1999

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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Published In

Science

DOI

ISSN

0036-8075

Publication Date

July 30, 1999

Volume

285

Issue

5428

Start / End Page

744 / 746

Location

United States

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

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Norris, J. D., Paige, L. A., Christensen, D. J., Chang, C. Y., Huacani, M. R., Fan, D., … McDonnell, D. P. (1999). Peptide antagonists of the human estrogen receptor. Science, 285(5428), 744–746. https://doi.org/10.1126/science.285.5428.744
Norris, J. D., L. A. Paige, D. J. Christensen, C. Y. Chang, M. R. Huacani, D. Fan, P. T. Hamilton, D. M. Fowlkes, and D. P. McDonnell. “Peptide antagonists of the human estrogen receptor.Science 285, no. 5428 (July 30, 1999): 744–46. https://doi.org/10.1126/science.285.5428.744.
Norris JD, Paige LA, Christensen DJ, Chang CY, Huacani MR, Fan D, et al. Peptide antagonists of the human estrogen receptor. Science. 1999 Jul 30;285(5428):744–6.
Norris, J. D., et al. “Peptide antagonists of the human estrogen receptor.Science, vol. 285, no. 5428, July 1999, pp. 744–46. Pubmed, doi:10.1126/science.285.5428.744.
Norris JD, Paige LA, Christensen DJ, Chang CY, Huacani MR, Fan D, Hamilton PT, Fowlkes DM, McDonnell DP. Peptide antagonists of the human estrogen receptor. Science. 1999 Jul 30;285(5428):744–746.
Journal cover image

Published In

Science

DOI

ISSN

0036-8075

Publication Date

July 30, 1999

Volume

285

Issue

5428

Start / End Page

744 / 746

Location

United States

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