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dc.contributor.authorDrouin, Len_US
dc.contributor.authorMcGrath, Sen_US
dc.contributor.authorVidler, LRen_US
dc.contributor.authorChaikuad, Aen_US
dc.contributor.authorMonteiro, Oen_US
dc.contributor.authorTallant, Cen_US
dc.contributor.authorPhilpott, Men_US
dc.contributor.authorRogers, Cen_US
dc.contributor.authorFedorov, Oen_US
dc.contributor.authorLiu, Men_US
dc.contributor.authorAkhtar, Wen_US
dc.contributor.authorHayes, Aen_US
dc.contributor.authorRaynaud, Fen_US
dc.contributor.authorMüller, Sen_US
dc.contributor.authorKnapp, Sen_US
dc.contributor.authorHoelder, Sen_US
dc.date.accessioned2020-07-28T14:12:43Z
dc.date.issued2015-03en_US
dc.identifier.citationJournal of medicinal chemistry, 2015, 58 (5), pp. 2553 - 2559en_US
dc.identifier.issn0022-2623en_US
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/3888
dc.identifier.eissn1520-4804en_US
dc.identifier.doi10.1021/jm501963een_US
dc.description.abstractThe bromodomain containing proteins BAZ2A/B play essential roles in chromatin remodeling and regulation of noncoding RNAs. We present the structure based discovery of a potent, selective, and cell active inhibitor 13 (BAZ2-ICR) of the BAZ2A/B bromodomains through rapid optimization of a weakly potent starting point. A key feature of the presented inhibitors is an intramolecular aromatic stacking interaction that efficiently occupies the shallow bromodomain pockets. 13 represents an excellent chemical probe for functional studies of the BAZ2 bromodomains in vitro and in vivo.en_US
dc.formatPrint-Electronicen_US
dc.format.extent2553 - 2559en_US
dc.languageengen_US
dc.language.isoengen_US
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/en_US
dc.subjectMicrosomesen_US
dc.subjectAnimalsen_US
dc.subjectMiceen_US
dc.subjectTriazolesen_US
dc.subjectChromosomal Proteins, Non-Histoneen_US
dc.subjectMolecular Probesen_US
dc.subjectMolecular Structureen_US
dc.subjectStructure-Activity Relationshipen_US
dc.subjectDrug Designen_US
dc.subjectModels, Molecularen_US
dc.titleStructure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.en_US
dc.typeJournal Article
rioxxterms.versionofrecord10.1021/jm501963een_US
rioxxterms.licenseref.startdate2015-03en_US
rioxxterms.typeJournal Article/Reviewen_US
dc.relation.isPartOfJournal of medicinal chemistryen_US
pubs.issue5en_US
pubs.notesNot knownen_US
pubs.organisational-group/ICR
pubs.organisational-group/ICR/Primary Group
pubs.organisational-group/ICR/Primary Group/ICR Divisions
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group)
pubs.organisational-group/ICR/Primary Group/ICR Divisions/Cancer Therapeutics/Medicinal Chemistry 4 (including Analytical Chemistry)
pubs.publication-statusPublisheden_US
pubs.volume58en_US
pubs.embargo.termsNot knownen_US
icr.researchteamClinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group)en_US
icr.researchteamMedicinal Chemistry 4 (including Analytical Chemistry)en_US
dc.contributor.icrauthorRaynaud, Florenceen_US
dc.contributor.icrauthorHoelder, Swenen_US


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Except where otherwise noted, this item's license is described as http://creativecommons.org/licenses/by/4.0/