dc.contributor.author | Drouin, L | |
dc.contributor.author | McGrath, S | |
dc.contributor.author | Vidler, LR | |
dc.contributor.author | Chaikuad, A | |
dc.contributor.author | Monteiro, O | |
dc.contributor.author | Tallant, C | |
dc.contributor.author | Philpott, M | |
dc.contributor.author | Rogers, C | |
dc.contributor.author | Fedorov, O | |
dc.contributor.author | Liu, M | |
dc.contributor.author | Akhtar, W | |
dc.contributor.author | Hayes, A | |
dc.contributor.author | Raynaud, F | |
dc.contributor.author | Müller, S | |
dc.contributor.author | Knapp, S | |
dc.contributor.author | Hoelder, S | |
dc.date.accessioned | 2020-07-28T14:12:43Z | |
dc.date.issued | 2015-03-12 | |
dc.identifier.citation | Journal of medicinal chemistry, 2015, 58 (5), pp. 2553 - 2559 | |
dc.identifier.issn | 0022-2623 | |
dc.identifier.uri | https://repository.icr.ac.uk/handle/internal/3888 | |
dc.identifier.eissn | 1520-4804 | |
dc.identifier.doi | 10.1021/jm501963e | |
dc.description.abstract | The 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.format | Print-Electronic | |
dc.format.extent | 2553 - 2559 | |
dc.language | eng | |
dc.language.iso | eng | |
dc.publisher | AMER CHEMICAL SOC | |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0 | |
dc.subject | Microsomes | |
dc.subject | Animals | |
dc.subject | Mice | |
dc.subject | Triazoles | |
dc.subject | Chromosomal Proteins, Non-Histone | |
dc.subject | Molecular Probes | |
dc.subject | Molecular Structure | |
dc.subject | Structure-Activity Relationship | |
dc.subject | Drug Design | |
dc.subject | Models, Molecular | |
dc.title | Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B. | |
dc.type | Journal Article | |
rioxxterms.versionofrecord | 10.1021/jm501963e | |
rioxxterms.licenseref.uri | https://creativecommons.org/licenses/by/4.0 | |
rioxxterms.licenseref.startdate | 2015-03 | |
rioxxterms.type | Journal Article/Review | |
dc.relation.isPartOf | Journal of medicinal chemistry | |
pubs.issue | 5 | |
pubs.notes | Not 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-status | Published | |
pubs.volume | 58 | |
pubs.embargo.terms | Not known | |
icr.researchteam | Clinical Pharmacology & Trials (including Drug Metabolism & Pharmacokinetics Group) | |
icr.researchteam | Medicinal Chemistry 4 (including Analytical Chemistry) | |
dc.contributor.icrauthor | Raynaud, Florence | |
dc.contributor.icrauthor | Hoelder, Swen | |