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Suppression of inflammation by a synthetic histone mimic

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. Rice, Jose M. Lora, Rab K. Prinjha, Kevin Lee (kevin.2.lee@gsk.com) and Alexander Tarakhovsky (tarakho@rockefeller.edu)
Additional contact information
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
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

Nature, 2010, vol. 468, issue 7327, 1119-1123

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.

Date: 2010
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DOI: 10.1038/nature09589

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