Peptide antagonists of the human estrogen receptor.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Norris, JD; Paige, LA; Christensen, DJ; Chang, CY; Huacani, MR; Fan, D; Hamilton, PT; Fowlkes, DM; McDonnell, DP

Published Date

  • July 30, 1999

Published In

Volume / Issue

  • 285 / 5428

Start / End Page

  • 744 - 746

PubMed ID

  • 10426998

International Standard Serial Number (ISSN)

  • 0036-8075

Digital Object Identifier (DOI)

  • 10.1126/science.285.5428.744


  • eng

Conference Location

  • United States