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dc.contributor.authorBamborough, Paulen
dc.contributor.authorChung, Chun-waen
dc.contributor.authorDemont, Emmanuel Hen
dc.contributor.authorFurze, Rebecca Cen
dc.contributor.authorBannister, Andrewen
dc.contributor.authorChe, Ka Hingen
dc.contributor.authorDiallo, Hawaen
dc.contributor.authorDouault, Clementen
dc.contributor.authorGrandi, Paolaen
dc.contributor.authorKouzarides, Tonyen
dc.contributor.authorMichon, Anne-Marieen
dc.contributor.authorMitchell, Darren Jen
dc.contributor.authorPrinjha, Rab Ken
dc.contributor.authorRau, Christinaen
dc.contributor.authorRobson, Samuelen
dc.contributor.authorSheppard, Robert Jen
dc.contributor.authorUpton, Richarden
dc.contributor.authorWatson, Robert Jen
dc.date.accessioned2020-03-10T17:04:47Z
dc.date.available2020-03-10T17:04:47Z
dc.date.issued2016-09-12en
dc.identifier.issn0044-8249
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/303269
dc.description.abstractATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.
dc.description.sponsorshipA.J.B., K.H.C., S.R. and T.K. acknowledge grants from Wellcome Trust (092096), Cancer Research UK (C6946/A14492, RG17001), and BBSRC (RG69031).
dc.languageenen
dc.publisherWiley
dc.titleA Chemical Probe for the ATAD2 Bromodomainen
dc.typeArticle
prism.endingPage11558
prism.issueIdentifier38en
prism.publicationDate2016en
prism.publicationNameAngewandte Chemieen
prism.startingPage11554
prism.volume128en
dc.identifier.doi10.17863/CAM.50354
dcterms.dateAccepted2016-08-17en
rioxxterms.versionofrecord10.1002/ange.201603928en
rioxxterms.versionAM*
rioxxterms.licenseref.urihttp://www.rioxx.net/licenses/all-rights-reserveden
rioxxterms.licenseref.startdate2016-09-12en
dc.contributor.orcidBannister, Andrew [0000-0002-6312-4436]
dc.contributor.orcidKouzarides, Tony [0000-0002-8918-4162]
rioxxterms.typeJournal Article/Reviewen
pubs.funder-project-idWellcome Trust (092096/Z/10/Z)
pubs.funder-project-idCancer Research UK (A14492)
cam.issuedOnline2016-08-17en


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