Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.

  title={Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.},
  author={F. Liu and D. Barsyte-Lovejoy and F. Li and Y. Xiong and Victoria K. Korboukh and X. Huang and Abdellah Allali-Hassani and W. Janzen and B. Roth and S. Frye and C. Arrowsmith and P. Brown and M. Vedadi and J. Jin},
  journal={Journal of medicinal chemistry},
  volume={56 21},
  • F. Liu, D. Barsyte-Lovejoy, +11 authors J. Jin
  • Published 2013
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • Among epigenetic "writers", "readers", and "erasers", the lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9me2) and nonhistone proteins, have been implicated in a variety of human diseases. A "toolkit" of well-characterized chemical probes will allow biological and disease hypotheses concerning these proteins to be tested in cell-based and animal models with high confidence. We previously discovered potent and selective G9a/GLP inhibitors… CONTINUE READING
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