IDEAS home Printed from https://ideas.repec.org/a/nat/nature/v468y2010i7327d10.1038_nature09589.html
   My bibliography  Save this article

Suppression of inflammation by a synthetic histone mimic

Author

Listed:
  • Edwige Nicodeme

    (Centre de Recherche GSK)

  • Kate L. Jeffrey

    (Laboratory of Lymphocyte Signaling, The Rockefeller University)

  • Uwe Schaefer

    (Laboratory of Lymphocyte Signaling, The Rockefeller University)

  • Soren Beinke

    (Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre)

  • Scott Dewell

    (Genomics Resource Center, The Rockefeller University)

  • Chun-wa Chung

    (GlaxoSmithKline R&D, Medicines Research Centre)

  • Rohit Chandwani

    (Laboratory of Lymphocyte Signaling, The Rockefeller University)

  • Ivan Marazzi

    (Laboratory of Lymphocyte Signaling, The Rockefeller University)

  • Paul Wilson

    (GlaxoSmithKline R&D, Medicines Research Centre)

  • Hervé Coste

    (Centre de Recherche GSK)

  • Julia White

    (GlaxoSmithKline R&D, Medicines Research Centre)

  • Jorge Kirilovsky

    (Centre de Recherche GSK)

  • Charles M. Rice

    (Laboratory of Virology and Infectious Disease, The Rockefeller University)

  • Jose M. Lora

    (Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre)

  • Rab K. Prinjha

    (Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre)

  • Kevin Lee

    (Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre)

  • Alexander Tarakhovsky

    (Laboratory of Lymphocyte Signaling, The Rockefeller University)

Abstract

Histone mimics target BET bromodomains Small molecules that perturb chromatin proteins are an emerging focus of current biomedical research. Two groups reporting in this issue have targeted bromodomain-containing BET proteins that bind acetylated lysine residues during gene activation, arriving at cell-permeable small molecule compounds with similar structures based on fused triazole-diazepine rings. James Bradner and colleagues report the development of a compound named JQ1. The BET protein BRD4, with two bromodomains, is implicated in human squamous cell carcinoma. JQ1 inhibits the growth of BRD4-dependent tumours in mouse models. Alexander Tarakhovsky and colleagues' inhibitor, I-BET, is shown to interfere with the binding of certain BET family members to acetylated histones. It inhibits activation of pro-inflammatory genes in macrophages and has immunomodulatory activity in a mouse model of inflammatory disease.

Suggested Citation

  • Edwige Nicodeme & Kate L. Jeffrey & Uwe Schaefer & Soren Beinke & Scott Dewell & Chun-wa Chung & Rohit Chandwani & Ivan Marazzi & Paul Wilson & Hervé Coste & Julia White & Jorge Kirilovsky & Charles M, 2010. "Suppression of inflammation by a synthetic histone mimic," Nature, Nature, vol. 468(7327), pages 1119-1123, December.
    • Handle: RePEc:nat:nature:v:468:y:2010:i:7327:d:10.1038_nature09589
    DOI: 10.1038/nature09589
    as

    Download full text from publisher

    File URL: https://www.nature.com/articles/nature09589
    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/nature09589?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.

    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:468:y:2010:i:7327:d:10.1038_nature09589. 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.