Helix mimetics as inhibitors of the interaction of the estrogen receptor with coactivator peptides

Jorge Becerril, Andrew D. Hamilton

Research output: Contribution to journalArticlepeer-review

Abstract

The short and curlies: A new α-helix mimetic based on a pyridylpyridone scaffold has been developed to bind to the estrogen receptor (ER) by mimicking the key leucine side chains of coactivator LXXLL boxes (L= leucine, X = any amino acid). These inhibitors compete with coactivator peptides for the surface of the ER and act as small-molecule inhibitors of the ER-coactivator interaction.

Original languageEnglish (US)
Pages (from-to)4471-4473
Number of pages3
JournalAngewandte Chemie - International Edition
Volume46
Issue number24
DOIs
StatePublished - 2007

Keywords

  • Amino acids -drug design
  • Inhibitors
  • Protein interactions
  • Proteomimetics

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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