Potent and selective bivalent inhibitors of BET bromodomains

Nature Chemical Biology

Volumn 12, Issue 12, 2016, Pages 1097-1104

  Waring, Michael J ^a,b   Chen, Huawei ^a   Rabow, Alfred A ^a   Walker, Graeme ^a   Bobby, Romel ^a   Boiko, Scott ^a   Bradbury, Rob H ^a   Callis, Rowena ^a   Clark, Edwin ^a   Dale, Ian ^a   Daniels, Danette L ^c   Dulak, Austin ^a   Flavell, Liz ^a   Holdgate, Geoff ^a   Jowitt, Thomas A ^d   Kikhney, Alexey ^e   McAlister, Mark ^a   Méndez, Jacqui ^c   Ogg, Derek ^a   Patel, Joe ^a   Petteruti, Philip ^a   Robb, Graeme R ^a   Robers, Matthew B ^c   Saif, Sakina ^a   Stratton, Natalie ^a   Svergun, Dmitri I ^e   Wang, Wenxian ^a   Whittaker, David ^a   Wilson, David M ^a   Yao, Yi ^a   more..

^a ASTRAZENECA   (United Kingdom)

^b NEWCASTLE UNIVERSITY   (United Kingdom)

^c PROMEGA CORPORATION   (United States)

^d UNIVERSITY OF MANCHESTER   (United Kingdom)

^e EUROPEAN MOLECULAR BIOLOGY LABORATORY   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

BROMODOMAIN CONTAINING PROTEIN 4; BROMODOMAIN INHIBITOR; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR BINDING PROTEIN; PROTEIN; UNCLASSIFIED DRUG; BRD4 PROTEIN, HUMAN; LIGAND; MOLECULAR LIBRARY; NUCLEAR PROTEIN; TRANSCRIPTION FACTOR;

ARTICLE; BINDING KINETICS; CONTROLLED STUDY; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SELECTIVITY; EC50; EMBRYO; HUMAN; HUMAN CELL; PRIORITY JOURNAL; ANTAGONISTS AND INHIBITORS; APOPTOSIS; CELL PROLIFERATION; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; ENZYME SPECIFICITY; METABOLISM; MOLECULAR LIBRARY; MOLECULAR MODEL; PHARMACOLOGY; PROTEIN DOMAIN; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE; X RAY CRYSTALLOGRAPHY;

APOPTOSIS; CELL LINE, TUMOR; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NUCLEAR PROTEINS; PROTEIN DOMAINS; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY; TRANSCRIPTION FACTORS;

EID: 84986242046     PISSN: 15524450     EISSN: 15524469     Source Type: Journal    
DOI: 10.1038/nchembio.2210     Document Type: Article

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