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Helix Mimetics as Inhibitors of the Interaction of the Estrogen Receptor with Coactivator Peptides
Author(s) -
Becerril Jorge,
Hamilton Andrew D.
Publication year - 2007
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200700657
Subject(s) - coactivator , helix (gastropod) , estrogen receptor , amino acid , leucine , chemistry , nuclear receptor coactivator 3 , biochemistry , computational biology , cancer research , biology , gene , genetics , transcription factor , cancer , ecology , snail , breast cancer
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.