An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.

  title={An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.},
  author={Kyle D. Konze and A. Ma and F. Li and D. Barsyte-Lovejoy and T. Parton and Christopher J Macnevin and F. Liu and C. Gao and X. Huang and E. Kuznetsova and Marie Rougi{\'e} and Alice Jiang and Samantha G Pattenden and Jacqueline L. Norris and L. James and B. Roth and P. Brown and S. Frye and C. Arrowsmith and K. Hahn and G. Wang and M. Vedadi and J. Jin},
  journal={ACS chemical biology},
  volume={8 6},
  • Kyle D. Konze, A. Ma, +20 authors J. Jin
  • Published 2013
  • Medicine, Biology
  • ACS chemical biology
  • EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a transcriptionally repressive post-translational modification. Overexpression of EZH2 and hypertrimethylation of H3K27 have been implicated in a number of cancers. Several selective inhibitors of EZH2 have been reported recently. Herein we disclose UNC1999, the first orally bioavailable inhibitor that has high in vitro… CONTINUE READING
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