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dc.contributor.authorChopra, Ren_US
dc.contributor.authorSadok, Aen_US
dc.contributor.authorCollins, Ien_US
dc.coverage.spatialEnglanden_US
dc.date.accessioned2019-02-22T14:55:22Z
dc.date.issued2019-04en_US
dc.identifierhttps://www.ncbi.nlm.nih.gov/pubmed/31200859en_US
dc.identifierS1740-6749(18)30016-7en_US
dc.identifier.citationDrug Discov Today Technol, 2019, 31 pp. 5 - 13en_US
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/3079
dc.identifier.eissn1740-6749en_US
dc.identifier.doi10.1016/j.ddtec.2019.02.002en_US
dc.description.abstractThere is a great deal of excitement around the concept of targeting proteins for degradation as an alternative to conventional inhibitory small molecules and antibodies. Protein degradation can be undertaken by bifunctional molecules that bind the target for ubiquitin mediated degradation by complexing them with Cereblon (CRBN), von Hippel-Lindau or other E-3 ligases. Alternatively, E-3 ligase receptors such as CRBN or DCAF15 can also be used as a 'template' to bind IMiD or sulphonamide like compounds to degrade multiple context specific proteins by the selected E-3 ligases. The 'template approach' results in the degradation of neo-substrates, some of which would be difficult to drug using conventional approaches. The chemical properties necessary for drug discovery, the rules by which neo-substrates are selected by E-3 ligase receptors and defining the optimal components of the ubiquitin proteasome for protein degradation are still to be fully elucidate. Theis review will aim to critically evaluate the different approaches and principles emerging for targted protein degradation.en_US
dc.format.extent5 - 13en_US
dc.languageengen_US
dc.language.isoengen_US
dc.rights.urihttps://creativecommons.org/licenses/by/4.0en_US
dc.titleA critical evaluation of the approaches to targeted protein degradation for drug discovery.en_US
dc.typeJournal Article
dcterms.dateAccepted2019-02-15en_US
rioxxterms.versionofrecord10.1016/j.ddtec.2019.02.002en_US
rioxxterms.licenseref.urihttps://creativecommons.org/licenses/by/4.0en_US
rioxxterms.licenseref.startdate2019-04en_US
rioxxterms.typeJournal Article/Reviewen_US
dc.relation.isPartOfDrug Discov Today Technolen_US
pubs.notesNo embargoen_US
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/Medicinal Chemistry 2
pubs.publication-statusPublisheden_US
pubs.volume31en_US
pubs.embargo.termsNo embargoen_US
icr.researchteamMedicinal Chemistry 2en_US
dc.contributor.icrauthorCollins, Ianen_US
dc.contributor.icrauthorChopra, Rajeshen_US


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