Discovery and development of potent and selective inhibitors of histone methyltransferase g9a
RF Sweis, M Pliushchev, PJ Brown, J Guo… - ACS medicinal …, 2014 - ACS Publications
ACS medicinal chemistry letters, 2014•ACS Publications
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.
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.
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.
ACS Publications