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.
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Becerril et al. (2007) studied this question.
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