Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains

Journal of the American Chemical Society

Volumn 136, Issue 26, 2014, Pages 9308-9319

  Hay, Duncan A ^a,b   Fedorov, Oleg ^b,c   Martin, Sarah ^b,c   Singleton, Dean C ^b,c   Tallant, Cynthia ^b,c   Wells, Christopher ^b,c   Picaud, Sarah ^b   Philpott, Martin ^b,c   Monteiro, Octovia P ^b,c   Rogers, Catherine M ^b,c   Conway, Stuart J ^a   Rooney, Timothy P C ^a   Tumber, Anthony ^b,c   Yapp, Clarence ^b,c   Filippakopoulos, Panagis ^b   Bunnage, Mark E ^d   Müller, Susanne ^b,c   Knapp, Stefan ^b,c   Schofield, Christopher J ^a   Brennan, Paul E ^b,c  

^a UNIVERSITY OF OXFORD   (United Kingdom)

^b UNIVERSITY OF OXFORD   (United Kingdom)

^c UNIVERSITY OF OXFORD   (United Kingdom)

^d PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMINO ACIDS; BINDING ENERGY; LEAD COMPOUNDS; MOLECULES;

CELLULAR ACTIVITIES; CREB BINDING PROTEINS; FLUORESCENCE RECOVERY; NANOMOLAR AFFINITY; PARALLEL SYNTHESIS; SMALL-MOLECULE INHIBITORS; THERAPEUTIC TARGETS; X RAY CRYSTAL STRUCTURES;

MOLECULAR BIOLOGY;

5 ISOXAZOLYL BENZIMIDAZOLE; ACYLTRANSFERASE; BENZIMIDAZOLE DERIVATIVE; CYCLIC AMP RESPONSIVE ELEMENT BINDING PROTEIN BINDING PROTEIN; HISTONE ACETYLTRANSFERASE PCAF; PROTEIN P53; UNCLASSIFIED DRUG; CREBBP PROTEIN, HUMAN; E1A ASSOCIATED P300 PROTEIN; EP300 PROTEIN, HUMAN; INDOLE DERIVATIVE; ISOXAZOLE DERIVATIVE; LIGAND; MOLECULAR LIBRARY;

AMINATION; ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING AFFINITY; BLEACHING; CELL ACTIVITY; CHEMICAL REACTION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG SYNTHESIS; FLUORESCENCE RECOVERY AFTER PHOTOBLEACHING; HUMAN; HUMAN CELL; NUCLEOTIDE SEQUENCE; OSTEOSARCOMA CELL; PROTEIN DOMAIN; REACTION OPTIMIZATION; SUZUKI REACTION; THERMOSTABILITY; X RAY CRYSTALLOGRAPHY; BINDING SITE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; DRUG SCREENING; GENETICS; HELA CELL LINE; LIVER MICROSOME; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; PROCEDURES; PROTEIN TERTIARY STRUCTURE; STRUCTURE ACTIVITY RELATION; SYNTHESIS; TUMOR SUPPRESSOR GENE;

BINDING SITES; CHEMISTRY TECHNIQUES, SYNTHETIC; CREB-BINDING PROTEIN; CRYSTALLOGRAPHY, X-RAY; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; E1A-ASSOCIATED P300 PROTEIN; FLUORESCENCE RECOVERY AFTER PHOTOBLEACHING; GENES, P53; HELA CELLS; HUMANS; INDOLES; ISOXAZOLES; LIGANDS; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN STRUCTURE, TERTIARY; SMALL MOLECULE LIBRARIES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84903739739     PISSN: 00027863     EISSN: 15205126     Source Type: Journal    
DOI: 10.1021/ja412434f     Document Type: Article

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