Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed

Show simple item record Yosaatmadja, Yuliana en Silva, S en Dickson, James en Patterson, Adam en Smaill, Jeffrey en Flanagan, Jack en McKeage, Mark en Squire, Christopher en 2016-08-05T01:14:35Z en 2015-12 en
dc.identifier.citation Journal of Structural Biology, 2015, 192 (3), pp. 539 - 544 en
dc.identifier.issn 1047-8477 en
dc.identifier.uri en
dc.description.abstract The discovery of genetic drivers of lung cancer in patient sub-groups has led to their use as predictive biomarkers and as targets for selective drug therapy. Some of the most important lung cancer drivers are mutations in the EGFR gene, for example, the exon 19 deletions and the L858R variant that confer sensitivity to the front line drugs erlotinib and gefitinib; the acquired T790M variants confer drug resistance and a poor prognosis. A challenge then in targeting EGFR is to produce drugs that inhibit both sensitising variants and resistance variants, leaving wild type protein in healthy cells unaffected. One such agent is AstraZeneca's "breakthrough" AZD9291 molecule that shows a 200-fold selectivity for T790M/L858R over wild type EGFR. Our X-ray crystal structure reveals the binding mode of AZD9291 to the kinase domain of wild type EGFR. en
dc.description.uri en
dc.publisher Elsevier en
dc.relation.ispartofseries Journal of Structural Biology en
dc.rights Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. Details obtained from en
dc.rights.uri en
dc.title Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed en
dc.type Journal Article en
dc.identifier.doi 10.1016/j.jsb.2015.10.018 en
pubs.issue 3 en
pubs.begin-page 539 en
pubs.volume 192 en
dc.rights.holder Copyright: Elsevier en
dc.identifier.pmid 26522274 en en
pubs.end-page 544 en
pubs.publication-status Published en
dc.rights.accessrights en
pubs.subtype Article en
pubs.elements-id 502972 en Medical and Health Sciences en Medical Sciences en Auckland Cancer Research en Pharmacology en Science en Biological Sciences en Science Research en Maurice Wilkins Centre (2010-2014) en
dc.identifier.eissn 1095-8657 en
pubs.record-created-at-source-date 2016-08-05 en
pubs.dimensions-id 26522274 en

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