A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction.

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作者： Timothy P C,Rooney ^[1] ; Panagis,Filippakopoulos ; Oleg,Fedorov ; Sarah,Picaud ; Wilian A,Cortopassi ; Duncan A,Hay ; Sarah,Martin ; Anthony,Tumber ; Catherine M,Rogers ; Martin,Philpott ; Minghua,Wang ; Amber L,Thompson ; Tom D,Heightman ; David C,Pryde ; Andrew,Cook ; Robert S,Paton ; Susanne,Müller ; Stefan,Knapp ; Paul E,Brennan ; Stuart J,Conway

作者单位： Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford, OX1 3TA (UK) http://conway.chem.ox.ac.uk/ ^[1]

关键词 CREBBP bromodomain enzyme inhibitors epigenetics ligand discovery

主题词 CREB结合蛋白质(CREB-Binding Protein);阳离子(Cations);表观基因组学(Epigenomics);配体(Ligands);模型, 分子(Models, Molecular);蛋白质结合(Protein Binding)

DOI 10.1002/anie.201402750

PMID 24821300

发布时间 2021-10-21

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