Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.

• Picaud S Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Fedorov O Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Thanasopoulou A Laboratory of Childhood Leukemia, Department of Biomedicine, University of Basel and Basel University Children's Hospital, Hebelstrasse 20 CH - 4031 Basel, Switzerland.
• Leonards K Laboratory of Childhood Leukemia, Department of Biomedicine, University of Basel and Basel University Children's Hospital, Hebelstrasse 20 CH - 4031 Basel, Switzerland.
• Jones K Epinova DPU, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.
• Meier J Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Olzscha H Laboratory of Cancer Biology, Department of Oncology, Medical Sciences Division, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, UK.
• Monteiro O Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Martin S Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Philpott M Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Tumber A Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Filippakopoulos P Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Yapp C Nuffield Department of Clinical Medicine, University of Oxford, Target Discovery Institute (TDI), Roosevelt Drive, Oxford OX3 7BN, UK.
• Wells C Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Che KH Gurdon Institute and Department of Pathology, University of Cambridge, Cambridge CB2 1QN, UK.
• Bannister A Gurdon Institute and Department of Pathology, University of Cambridge, Cambridge CB2 1QN, UK.
• Robson S Gurdon Institute and Department of Pathology, University of Cambridge, Cambridge CB2 1QN, UK.
• Kumar U Epinova DPU, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.
• Parr N Epinova DPU, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.
• Lee K Epinova DPU, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.
• Lugo D Experimental Medicines Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK.
• Jeffrey P Experimental Medicines Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK.
• Taylor S Experimental Medicines Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, UK.
• Vecellio ML Nuffield Department of Clinical Medicine, University of Oxford, Target Discovery Institute (TDI), Roosevelt Drive, Oxford OX3 7BN, UK.
• Bountra C Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Brennan PE Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• O'Mahony A BioSeek Division of DiscoveRx Corporation, 310 Utah Street, Suite 100, South San Francisco, CA, 94080, USA.
• Velichko S BioSeek Division of DiscoveRx Corporation, 310 Utah Street, Suite 100, South San Francisco, CA, 94080, USA.
• Müller S Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.
• Hay D Nuffield Department of Clinical Medicine, University of Oxford, Target Discovery Institute (TDI), Roosevelt Drive, Oxford OX3 7BN, UK.
• Daniels DL Promega Corporation, 2800 Woods Hollow Road, Madison, Wisconsin, U.S.A 53711.
• Urh M Promega Corporation, 2800 Woods Hollow Road, Madison, Wisconsin, U.S.A 53711.
• La Thangue NB Laboratory of Cancer Biology, Department of Oncology, Medical Sciences Division, University of Oxford, Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, UK.
• Kouzarides T Gurdon Institute and Department of Pathology, University of Cambridge, Cambridge CB2 1QN, UK.
• Prinjha R Epinova DPU, Immuno-Inflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage SG1 2NY, UK.
• Schwaller J Laboratory of Childhood Leukemia, Department of Biomedicine, University of Basel and Basel University Children's Hospital, Hebelstrasse 20 CH - 4031 Basel, Switzerland.
• Knapp S Nuffield Department of Clinical Medicine, University of Oxford, Structural Genomics Consortium, Old Road Campus Research Building, Roosevelt Drive, Oxford OX3 7DQ, UK.

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Amino Acid Sequence

Animals

Antineoplastic Combined Chemotherapy Protocols

Cell Line, Tumor

Doxorubicin

Drug Synergism

Enzyme Inhibitors

Humans

Leukemia, Myeloid, Acute

Mice

Models, Molecular

Molecular Sequence Data

Oxazepines

Protein Structure, Tertiary

Xenograft Model Antitumor Assays

p300-CBP Transcription Factors