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Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain.
Chaikuad, Apirat; Lang, Steffen; Brennan, Paul E; Temperini, Claudia; Fedorov, Oleg; Hollander, Johan; Nachane, Ruta; Abell, Chris; Müller, Susanne; Siegal, Gregg; Knapp, Stefan.
Afiliación
  • Chaikuad A; Nuffield Department of Clinical Medicine, Structural Genomics Consortium and Target Discovery Institute, University of Oxford , Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, U.K.
  • Lang S; Department of Chemistry, University of Cambridge , Lensfield Road, Cambridge CB2 1EW, U.K.
  • Brennan PE; Nuffield Department of Clinical Medicine, Structural Genomics Consortium and Target Discovery Institute, University of Oxford , Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, U.K.
  • Temperini C; Leiden Institute of Chemistry, Leiden University , Einsteinweg 55, 2333 CC Leiden, Netherlands.
  • Fedorov O; Nuffield Department of Clinical Medicine, Structural Genomics Consortium and Target Discovery Institute, University of Oxford , Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, U.K.
  • Hollander J; ZoBio , Einsteinweg 55, 2333 CC Leiden, Netherlands.
  • Nachane R; ZoBio , Einsteinweg 55, 2333 CC Leiden, Netherlands.
  • Abell C; Department of Chemistry, University of Cambridge , Lensfield Road, Cambridge CB2 1EW, U.K.
  • Müller S; Nuffield Department of Clinical Medicine, Structural Genomics Consortium and Target Discovery Institute, University of Oxford , Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, U.K.
  • Siegal G; ZoBio , Einsteinweg 55, 2333 CC Leiden, Netherlands.
  • Knapp S; Nuffield Department of Clinical Medicine, Structural Genomics Consortium and Target Discovery Institute, University of Oxford , Old Road Campus Research Building, Roosevelt Drive, Oxford, OX3 7DQ, U.K.
J Med Chem ; 59(4): 1648-53, 2016 Feb 25.
Article en En | MEDLINE | ID: mdl-26731131
The P300/CBP-associated factor plays a central role in retroviral infection and cancer development, and the C-terminal bromodomain provides an opportunity for selective targeting. Here, we report several new classes of acetyl-lysine mimetic ligands ranging from mM to low micromolar affinity that were identified using fragment screening approaches. The binding modes of the most attractive fragments were determined using high resolution crystal structures providing chemical starting points and structural models for the development of potent and selective PCAF inhibitors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Factores de Transcripción p300-CBP / Bibliotecas de Moléculas Pequeñas Tipo de estudio: Diagnostic_studies / Prognostic_studies / Risk_factors_studies Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Factores de Transcripción p300-CBP / Bibliotecas de Moléculas Pequeñas Tipo de estudio: Diagnostic_studies / Prognostic_studies / Risk_factors_studies Límite: Humans Idioma: En Revista: J Med Chem Asunto de la revista: QUIMICA Año: 2016 Tipo del documento: Article Pais de publicación: Estados Unidos