Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia

Mark A. Dawson (), Rab K. Prinjha, Antje Dittmann, George Giotopoulos, Marcus Bantscheff, Wai-In Chan, Samuel C. Robson, Chun-wa Chung, Carsten Hopf, Mikhail M. Savitski, Carola Huthmacher, Emma Gudgin, Dave Lugo, Soren Beinke, Trevor D. Chapman, Emma J. Roberts, Peter E. Soden, Kurt R. Auger, Olivier Mirguet, Konstanze Doehner, Ruud Delwel, Alan K. Burnett, Phillip Jeffrey, Gerard Drewes, Kevin Lee, Brian J. P. Huntly () and Tony Kouzarides ()
Additional contact information
Mark A. Dawson: Cambridge Institute for Medical Research and Addenbrookes Hospital, University of Cambridge
Rab K. Prinjha: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Antje Dittmann: Cellzome AG Meyerhofstrasse 1
George Giotopoulos: Cambridge Institute for Medical Research and Addenbrookes Hospital, University of Cambridge
Marcus Bantscheff: Cellzome AG Meyerhofstrasse 1
Wai-In Chan: Cambridge Institute for Medical Research and Addenbrookes Hospital, University of Cambridge
Samuel C. Robson: Gurdon Institute and Department of Pathology
Chun-wa Chung: Molecular Discovery Research, GlaxoSmithKline R&D
Carsten Hopf: Cellzome AG Meyerhofstrasse 1
Mikhail M. Savitski: Cellzome AG Meyerhofstrasse 1
Carola Huthmacher: Cellzome AG Meyerhofstrasse 1
Emma Gudgin: Cambridge Institute for Medical Research and Addenbrookes Hospital, University of Cambridge
Dave Lugo: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Soren Beinke: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Trevor D. Chapman: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Emma J. Roberts: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Peter E. Soden: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Kurt R. Auger: Cancer Epigenetics DPU, Oncology R&D, GlaxoSmithKline, 1250 South Collegeville Road
Olivier Mirguet: Lipid Metabolism Discovery Performance Unit, GSK R&D
Konstanze Doehner: University Hospital of Ulm Internal Medicine III Albert- Einstein-Allee 23
Ruud Delwel: Erasmus University Medical Center
Alan K. Burnett: Cardiff University School of Medicine
Phillip Jeffrey: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Gerard Drewes: Cellzome AG Meyerhofstrasse 1
Kevin Lee: Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre
Brian J. P. Huntly: Cambridge Institute for Medical Research and Addenbrookes Hospital, University of Cambridge
Tony Kouzarides: Gurdon Institute and Department of Pathology

Nature, 2011, vol. 478, issue 7370, 529-533

Abstract: BET proteins as targets in mixed lineage leukaemia Rearrangements of the MLL (mixed lineage leukaemia) gene, and chimaeric MLL-fusion proteins, occur in a number of aggressive leukaemias including acute myeloid leukemia (AML). Tony Kouzarides and colleagues now find that MLL-fusion proteins are associated with BET family proteins in transcription factor complexes. GSK1210151A (I-BET151), a new small-molecule inhibitor of the interaction between BET family proteins and specific chromatin marks, is shown to have efficacy against AML cells in vitro and in mouse models, suggesting a new therapeutic strategy for AML.

Date: 2011
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DOI: 10.1038/nature10509

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