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dc.contributor.authorScott, Duncan E
dc.contributor.authorRooney, Timothy PC
dc.contributor.authorBayle, Elliott D
dc.contributor.authorMirza, Tashfina
dc.contributor.authorWillems, Henriette MG
dc.contributor.authorClarke, Jonathan H
dc.contributor.authorAndrews, Stephen P
dc.contributor.authorSkidmore, John
dc.date.accessioned2020-06-12T23:30:24Z
dc.date.available2020-06-12T23:30:24Z
dc.date.issued2020-08-13
dc.identifier.issn1948-5875
dc.identifier.urihttps://www.repository.cam.ac.uk/handle/1810/306747
dc.description.abstractBifunctional molecules known as PROTACs simultaneously bind an E3 ligase and a protein of interest to direct ubiquitination and clearance of that protein, and they have emerged in the past decade as an exciting new paradigm in drug discovery. In order to investigate the permeability and properties of these large molecules, we synthesized two panels of PROTAC molecules, constructed from a range of protein-target ligands, linkers, and E3 ligase ligands. The androgen receptor, which is a well-studied protein in the PROTAC field was used as a model system. The physicochemical properties and permeability of PROTACs are discussed.
dc.description.sponsorshipThis work was funded by Alzheimer’s Research UK (grant: ARUK-2015DDI-CAM), with support from the ALBORADA Trust. The ALBORADA Drug Discovery Institute is core funded by Alzheimer’s Research UK (registered charity No. 1077089 and SC042474).
dc.format.mediumElectronic-eCollection
dc.languageeng
dc.publisherAmerican Chemical Society (ACS)
dc.rightsAll rights reserved
dc.titleSystematic Investigation of the Permeability of Androgen Receptor PROTACs.
dc.typeArticle
prism.endingPage1547
prism.issueIdentifier8
prism.publicationDate2020
prism.publicationNameACS Med Chem Lett
prism.startingPage1539
prism.volume11
dc.identifier.doi10.17863/CAM.53835
dcterms.dateAccepted2020-06-01
rioxxterms.versionofrecord10.1021/acsmedchemlett.0c00194
rioxxterms.versionAM
rioxxterms.licenseref.urihttp://www.rioxx.net/licenses/all-rights-reserved
rioxxterms.licenseref.startdate2020-08
dc.contributor.orcidScott, Duncan [0000-0003-1917-9576]
dc.contributor.orcidRooney, Timothy [0000-0001-6788-5526]
dc.contributor.orcidWillems, Henriette [0000-0001-7196-5975]
dc.contributor.orcidClarke, Jonathan [0000-0002-4079-5333]
dc.contributor.orcidAndrews, Stephen [0000-0001-6021-6899]
dc.contributor.orcidSkidmore, John [0000-0001-9108-7858]
dc.identifier.eissn1948-5875
rioxxterms.typeJournal Article/Review
pubs.funder-project-idAlzheimer's Research UK (ARUK-2015DDI-CAM)
cam.issuedOnline2020-06-08
cam.orpheus.successTue Jun 16 10:39:04 BST 2020 - Embargo updated
rioxxterms.freetoread.startdate2021-06-08


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