Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.

@article{Knutson2014SelectiveIO,
  title={Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.},
  author={Sarah K. Knutson and Satoshi Kawano and Yukinori Minoshima and Natalie M. Warholic and K Huang and Yonghong Xiao and Tadashi Kadowaki and Mai Uesugi and Galina Kuznetsov and Namita Kumar and Tim J. Wigle and Christine R. Klaus and Christina J. Allain and Alejandra Raimondi and Nigel J. Waters and Jesse J. Smith and Margaret Porter-Scott and Richard Chesworth and Mikel P. Moyer and Robert A Copeland and Victoria M. Richon and Toshimitsu Uenaka and Roy M. Pollock and Kevin W. Kuntz and Akira Yokoi and Heike Keilhack},
  journal={Molecular cancer therapeutics},
  year={2014},
  volume={13 4},
  pages={842-54}
}
Mutations within the catalytic domain of the histone methyltransferase EZH2 have been identified in subsets of patients with non-Hodgkin lymphoma (NHL). These genetic alterations are hypothesized to confer an oncogenic dependency on EZH2 enzymatic activity in these cancers. We have previously reported the discovery of EPZ005678 and EPZ-6438, potent and selective S-adenosyl-methionine-competitive small molecule inhibitors of EZH2. Although both compounds are similar with respect to their… CONTINUE READING
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