Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.

2014 
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.
    • Correction
    • Source
    • Cite
    • Save
    • Machine Reading By IdeaReader
    23
    References
    113
    Citations
    NaN
    KQI
    []
    Baidu
    map