Modulation of human estrogen receptor α activity by multivalent estradiol-peptidomimetic conjugates

Justin M. Holub, Michael J. Garabedian, Kent Kirshenbaum

Research output: Contribution to journalArticle

Abstract

Estradiol-peptidomimetic conjugates (EPCs) are linear, sequence-specific peptoid oligomers that site-specifically display multiple copies of 17β-estradiol (E2), a ligand for the human estrogen receptor α (hERα). We evaluate the ability of multivalent EPCs to activate hERα-mediated transcription. EPCs activated the hERα in both a length- and valence-dependent manner, with the highest levels of activation generated by divalent peptoid 6-mers, divalent 18-mers, and trivalent 9-mers. Hexavalent EPCs did not activate hERα, but instead blocked E2-mediated hERα activation. The physicochemical features of EPCs can be precisely tuned, which may allow the generation of a library of chemical tools for modulating specific effects of estrogens.

Original languageEnglish (US)
Pages (from-to)337-345
Number of pages9
JournalMolecular BioSystems
Volume7
Issue number2
DOIs
StatePublished - Feb 1 2011

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Biology

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