Show simple item record

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.issued2015-03
dc.identifier.citationJournal of medicinal chemistry, 2015, 58 (5), pp. 2553 - 2559
dc.identifier.issn0022-2623
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/3888
dc.identifier.eissn1520-4804
dc.identifier.doi10.1021/jm501963e
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.
dc.formatPrint-Electronic
dc.format.extent2553 - 2559
dc.languageeng
dc.language.isoeng
dc.rights.urihttps://creativecommons.org/licenses/by/4.0
dc.subjectMicrosomes
dc.subjectAnimals
dc.subjectMice
dc.subjectTriazoles
dc.subjectChromosomal Proteins, Non-Histone
dc.subjectMolecular Probes
dc.subjectMolecular Structure
dc.subjectStructure-Activity Relationship
dc.subjectDrug Design
dc.subjectModels, Molecular
dc.titleStructure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.
dc.typeJournal Article
rioxxterms.versionofrecord10.1021/jm501963e
rioxxterms.licenseref.urihttps://creativecommons.org/licenses/by/4.0
rioxxterms.licenseref.startdate2015-03
rioxxterms.typeJournal Article/Review
dc.relation.isPartOfJournal of medicinal chemistry
pubs.issue5
pubs.notesNot known
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-statusPublished
pubs.volume58
pubs.embargo.termsNot known
icr.researchteamClinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group)en_US
icr.researchteamMedicinal Chemistry 4 (including Analytical Chemistry)en_US
dc.contributor.icrauthorRaynaud, Florenceen
dc.contributor.icrauthorHoelder, Swenen


Files in this item

Thumbnail

This item appears in the following collection(s)

Show simple item record

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