EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

Michael T. McCabe, Heidi M. Ott, Gopinath Ganji, Susan Korenchuk, Christine Thompson, Glenn S. Van Aller, Yan Liu, Alan P. Graves, Anthony Della Pietra, Elsie Diaz, Louis V. LaFrance, Mark Mellinger, Celine Duquenne, Xinrong Tian, Ryan G. Kruger, Charles F. McHugh, Martin Brandt, William H. Miller, Dashyant Dhanak, Sharad K. Verma, Peter J. Tummino and Caretha L. Creasy ()
Additional contact information
Michael T. McCabe: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Heidi M. Ott: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Gopinath Ganji: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Susan Korenchuk: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Christine Thompson: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Glenn S. Van Aller: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Yan Liu: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Alan P. Graves: Platform Technology and Sciences, GlaxoSmithKline, 1250 S. Collegeville Road
Anthony Della Pietra: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Elsie Diaz: Platform Technology and Sciences, GlaxoSmithKline, 1250 S. Collegeville Road
Louis V. LaFrance: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Mark Mellinger: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Celine Duquenne: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Xinrong Tian: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Ryan G. Kruger: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Charles F. McHugh: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Martin Brandt: Platform Technology and Sciences, GlaxoSmithKline, 1250 S. Collegeville Road
William H. Miller: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Dashyant Dhanak: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Sharad K. Verma: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Peter J. Tummino: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road
Caretha L. Creasy: Cancer Epigenetics Discovery Performance Unit, Cancer Research, Oncology R&D, GlaxoSmithKline, 1250 S. Collegeville Road

Nature, 2012, vol. 492, issue 7427, 108-112

Abstract: EZH2 is a methyltransferase that is mutated in lymphoma; here a potent small molecule inhibitor of EZH2 is described, which inhibits the proliferation of EZH2 mutant cell lines and growth of EZH2 mutant xenografts in mice, thus providing a potential treatment for EZH2 mutant lymphoma.

Date: 2012
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DOI: 10.1038/nature11606

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