EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.

  title={EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity.},
  author={John E Campbell and Kevin W. Kuntz and Sarah K. Knutson and Natalie M. Warholic and Heike Keilhack and Tim J. Wigle and Alejandra Raimondi and Christine R. Klaus and Nathalie Rioux and Akira Yokoi and Satoshi Kawano and Yukinori Minoshima and Hyeong-Wook Choi and Margaret Porter Scott and Nigel J. Waters and Jesse J. Smith and Richard Chesworth and Mikel P. Moyer and Robert A Copeland},
  journal={ACS medicinal chemistry letters},
  volume={6 5},
Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with… CONTINUE READING


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