IDEAS home Printed from https://ideas.repec.org/a/nat/nature/v488y2012i7411d10.1038_nature11262.html
   My bibliography  Save this article

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
    as

    Download full text from publisher

    File URL: https://www.nature.com/articles/nature11262
    File Function: Abstract
    Download Restriction: Access to the full text of the articles in this series is restricted.
    File URL: https://libkey.io/10.1038/nature11262?utm_source=ideas
    LibKey link: if access is restricted and if your library uses this service, LibKey will redirect you to where you can use your library subscription to access this item
    ---><---

    As the access to this document is restricted, you may want to search for a different version of it.

    Citations

    Citations are extracted by the CitEc Project, subscribe to its RSS feed for this item.
    as


    Cited by:

    1. 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.
    2. 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.
    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.

    More about this item

    Statistics

    Access and download statistics

    Corrections

    All material on this site has been provided by the respective publishers and authors. You can help correct errors and omissions. When requesting a correction, please mention this item's handle: RePEc:nat:nature:v:488:y:2012:i:7411:d:10.1038_nature11262. See general information about how to correct material in RePEc.

    If you have authored this item and are not yet registered with RePEc, we encourage you to do it here. This allows to link your profile to this item. It also allows you to accept potential citations to this item that we are uncertain about.

    We have no bibliographic references for this item. You can help adding them by using this form .

    If you know of missing items citing this one, you can help us creating those links by adding the relevant references in the same way as above, for each refering item. If you are a registered author of this item, you may also want to check the "citations" tab in your RePEc Author Service profile, as there may be some citations waiting for confirmation.

    For technical questions regarding this item, or to correct its authors, title, abstract, bibliographic or download information, contact: Sonal Shukla or Springer Nature Abstracting and Indexing (email available below). General contact details of provider: http://www.nature.com .

    Please note that corrections may take a couple of weeks to filter through the various RePEc services.

    IDEAS is a RePEc service. RePEc uses bibliographic data supplied by the respective publishers.