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

Jorge Becerril; Andrew D. Hamilton

doi:10.1002/anie.200700657

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

Jorge Becerril, Andrew D. Hamilton

Chemistry

Research output: Contribution to journal › Article › peer-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 language	English (US)
Pages (from-to)	4471-4473
Number of pages	3
Journal	Angewandte Chemie - International Edition
Volume	46
Issue number	24
DOIs	https://doi.org/10.1002/anie.200700657
State	Published - 2007

Keywords

Amino acids -drug design
Inhibitors
Protein interactions
Proteomimetics

ASJC Scopus subject areas

Catalysis
General Chemistry

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10.1002/anie.200700657

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

Abstract

Keywords

ASJC Scopus subject areas

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