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A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response

Author

Listed:
  • Laurens Kruidenier

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Chun-wa Chung

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Zhongjun Cheng

    (Memorial Sloan-Kettering Cancer Center, 1275 York Avenue)

  • John Liddle

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • KaHing Che

    (Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
    Botnar Research Centre, NIHR Biomedical Research Unit, University of Oxford OX3 7LD)

  • Gerard Joberty

    (Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany)

  • Marcus Bantscheff

    (Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany)

  • Chas Bountra

    (Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK)

  • Angela Bridges

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Hawa Diallo

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Dirk Eberhard

    (Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany)

  • Sue Hutchinson

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Emma Jones

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Roy Katso

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Melanie Leveridge

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Palwinder K. Mander

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Julie Mosley

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Cesar Ramirez-Molina

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Paul Rowland

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Christopher J. Schofield

    (Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK)

  • Robert J. Sheppard

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Julia E. Smith

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Catherine Swales

    (Botnar Research Centre, NIHR Biomedical Research Unit, University of Oxford OX3 7LD)

  • Robert Tanner

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Pamela Thomas

    (Platform Technology and Science, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

  • Anthony Tumber

    (Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK)

  • Gerard Drewes

    (Cellzome AG, Meyerhofstrasse 1, 69117 Heidelberg, Germany)

  • Udo Oppermann

    (Structural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Headington OX3 7DQ, UK
    Botnar Research Centre, NIHR Biomedical Research Unit, University of Oxford OX3 7LD)

  • Dinshaw J. Patel

    (Memorial Sloan-Kettering Cancer Center, 1275 York Avenue)

  • Kevin Lee

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK
    Present address: Pfizer, Biotherapeutics R&D, 200 Cambridgepark Drive, Cambridge, Massachusetts 02140, USA.)

  • David M. Wilson

    (Epinova DPU, Immuno-Inflammation Therapy Area, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage SG1 2NY, UK)

Abstract

A structure-guided small-molecule and chemoproteomics approach uncovers a catalytic site inhibitor selective for the jumonji subfamily of H3K27me3 demethylases; the inhibitor decreases lipopolysaccharide-induced proinflammatory cytokine production by human primary macrophages.

Suggested Citation

  • Laurens Kruidenier & Chun-wa Chung & Zhongjun Cheng & John Liddle & KaHing Che & Gerard Joberty & Marcus Bantscheff & Chas Bountra & Angela Bridges & Hawa Diallo & Dirk Eberhard & Sue Hutchinson & Emm, 2012. "A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response," Nature, Nature, vol. 488(7411), pages 404-408, August.
    • Handle: RePEc:nat:nature:v:488:y:2012:i:7411:d:10.1038_nature11262
    DOI: 10.1038/nature11262
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    Cited by:

    1. Thaddeus J. Kunkel & Alice Townsend & Kyle A. Sullivan & Jean Merlet & Edward H. Schuchman & Daniel A. Jacobson & Andrew P. Lieberman, 2023. "The cholesterol transporter NPC1 is essential for epigenetic regulation and maturation of oligodendrocyte lineage cells," Nature Communications, Nature, vol. 14(1), pages 1-17, December.
    2. Jayden Sterling & Jennifer R. Baker & Adam McCluskey & Lenka Munoz, 2023. "Systematic literature review reveals suboptimal use of chemical probes in cell-based biomedical research," Nature Communications, Nature, vol. 14(1), pages 1-12, December.
    3. Alexandra D’Oto & Jie Fang & Hongjian Jin & Beisi Xu & Shivendra Singh & Anoushka Mullasseril & Victoria Jones & Ahmed Abu-Zaid & Xinyu Buttlar & Bailey Cooke & Dongli Hu & Jason Shohet & Andrew J. Mu, 2021. "KDM6B promotes activation of the oncogenic CDK4/6-pRB-E2F pathway by maintaining enhancer activity in MYCN-amplified neuroblastoma," Nature Communications, Nature, vol. 12(1), pages 1-19, December.

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