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Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
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Discovery and development of potent and selective inhibitors of histone methyltransferase g9a
Ramzi F Sweis1, Marina Pliushchev1, Peter J Brown2
1Discovery Research, AbbVie Inc. , 1 North Waukegan Road, North Chicago, Illinois 60064, United States.
ACS Medicinal Chemistry Letters
|June 6, 2014
Abstract:
G9a is a histone lysine methyltransferase responsible for the methylation of histone H3 lysine 9. The discovery of A-366 arose from a unique diversity screening hit, which was optimized by incorporation of a propyl-pyrrolidine subunit to occupy the enzyme lysine channel. A-366 is a potent inhibitor of G9a (IC50: 3.3 nM) with greater than 1000-fold selectivity over 21 other methyltransferases.
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