Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.

@article{Xu2015SelectiveIO,
  title={Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.},
  author={Bowen Xu and D. On and Anqi Ma and T. Parton and Kyle D. Konze and Samantha G Pattenden and David F. Allison and L. Cai and Shira Rockowitz and Shichong Liu and Y. Liu and F. Li and M. Vedadi and S. Frye and B. Garcia and D. Zheng and J. Jin and G. Wang},
  journal={Blood},
  year={2015},
  volume={125 2},
  pages={
          346-57
        }
}
Enhancer of zeste homolog 2 (EZH2) and related EZH1 control gene expression and promote tumorigenesis via methylating histone H3 at lysine 27 (H3K27). These methyltransferases are ideal therapeutic targets due to their frequent hyperactive mutations and overexpression found in cancer, including hematopoietic malignancies. Here, we characterized a set of small molecules that allow pharmacologic manipulation of EZH2 and EZH1, which include UNC1999, a selective inhibitor of both enzymes, and… Expand
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