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Design, Synthesis, and Biological Evaluation of a Small‐Molecule Inhibitor of the Histone Acetyltransferase Gcn5
Author(s) -
Biel Markus,
Kretsovali Androniki,
Karatzali Efthymia,
Papamatheakis Joseph,
Giannis Athanassios
Publication year - 2004
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.200453879
Subject(s) - histone acetyltransferase , acetylation , acetyltransferase , histone , computer science , chemistry , histone acetyltransferases , computational biology , biochemistry , biology , gene
HATs off! The development of the first cell‐permeable small‐molecule inhibitor of the human histone acetyltransferase (HAT) Gcn5 opens up new possibilities for understanding the histone code. Based on kinetic data and the proposed mechanism of the acetylation by Gcn5, the relatively simple butyrolactone structure of the inhibitor was identified.