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

Author

Listed:
  • 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 III

    (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)

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.

Suggested Citation

  • Michael T. McCabe & Heidi M. Ott & Gopinath Ganji & Susan Korenchuk & Christine Thompson & Glenn S. Van Aller & Yan Liu & Alan P. Graves & Anthony Della Pietra III & Elsie Diaz & Louis V. LaFrance & M, 2012. "EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations," Nature, Nature, vol. 492(7427), pages 108-112, December.
    • Handle: RePEc:nat:nature:v:492:y:2012:i:7427:d:10.1038_nature11606
    DOI: 10.1038/nature11606
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    Citations

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    Cited by:

    1. Wen Hao Neo & Yiran Meng & Alba Rodriguez-Meira & Muhammad Z. H. Fadlullah & Christopher A. G. Booth & Emanuele Azzoni & Supat Thongjuea & Marella F. T. R. Bruijn & Sten Eirik W. Jacobsen & Adam J. Me, 2021. "Ezh2 is essential for the generation of functional yolk sac derived erythro-myeloid progenitors," Nature Communications, Nature, vol. 12(1), pages 1-12, December.
    2. Ayushi Verma & Akhilesh Singh & Manish Pratap Singh & Mushtaq Ahmad Nengroo & Krishan Kumar Saini & Saumya Ranjan Satrusal & Muqtada Ali Khan & Priyank Chaturvedi & Abhipsa Sinha & Sanjeev Meena & Anu, 2022. "EZH2-H3K27me3 mediated KRT14 upregulation promotes TNBC peritoneal metastasis," Nature Communications, Nature, vol. 13(1), pages 1-22, December.
    3. Carolina Gracia-Diaz & Yijing Zhou & Qian Yang & Reza Maroofian & Paula Espana-Bonilla & Chul-Hwan Lee & Shuo Zhang & Natàlia Padilla & Raquel Fueyo & Elisa A. Waxman & Sunyimeng Lei & Garrett Otrimsk, 2023. "Gain and loss of function variants in EZH1 disrupt neurogenesis and cause dominant and recessive neurodevelopmental disorders," Nature Communications, Nature, vol. 14(1), pages 1-18, December.
    4. Xiao Chen & Yinglu Li & Fang Zhu & Xinjing Xu & Brian Estrella & Manuel A. Pazos & John T. McGuire & Dimitris Karagiannis & Varun Sahu & Mustafo Mustafokulov & Claudio Scuoppo & Francisco J. Sánchez-R, 2023. "Context-defined cancer co-dependency mapping identifies a functional interplay between PRC2 and MLL-MEN1 complex in lymphoma," Nature Communications, Nature, vol. 14(1), pages 1-17, December.
    5. Lin Zhang & Jingkun Qu & Yutao Qi & Yimin Duan & Yu-Wen Huang & Zhifen Zhou & Ping Li & Jun Yao & Beibei Huang & Shuxing Zhang & Dihua Yu, 2022. "EZH2 engages TGFβ signaling to promote breast cancer bone metastasis via integrin β1-FAK activation," Nature Communications, Nature, vol. 13(1), pages 1-16, December.
    6. Pauliina M. Munne & Lahja Martikainen & Iiris Räty & Kia Bertula & Nonappa & Janika Ruuska & Hanna Ala-Hongisto & Aino Peura & Babette Hollmann & Lilya Euro & Kerim Yavuz & Linda Patrikainen & Maria S, 2021. "Compressive stress-mediated p38 activation required for ERα + phenotype in breast cancer," Nature Communications, Nature, vol. 12(1), pages 1-17, December.
    7. Jiangtao Ren & Zheng Sun & Shuang Zhao & Jinyuan Huang & Yukun Wang & Cheng Zhang & Jinhai Huang & Chenhao Zhang & Ruipu Zhang & Zhihan Zhang & Xu Ji & Zhihui Shao, 2024. "Enantioselective synthesis of chiral α,α-dialkyl indoles and related azoles by cobalt-catalyzed hydroalkylation and regioselectivity switch," Nature Communications, Nature, vol. 15(1), pages 1-14, December.

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