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dc.contributor.authorMiller, DSJ
dc.contributor.authorVoell, SA
dc.contributor.authorSosič, I
dc.contributor.authorProj, M
dc.contributor.authorRossanese, OW
dc.contributor.authorSchnakenburg, G
dc.contributor.authorGütschow, M
dc.contributor.authorCollins, I
dc.contributor.authorSteinebach, C
dc.date.accessioned2022-05-18T09:58:14Z
dc.date.available2022-05-18T09:58:14Z
dc.date.issued2022-06-22
dc.identifier.citationRSC Medicinal Chemistry
dc.identifier.urihttps://repository.icr.ac.uk/handle/internal/5136
dc.identifier.eissn2632-8682
dc.identifier.eissn2632-8682
dc.identifier.doi10.1039/d2md00064d
dc.identifier.doi10.1039/d2md00064d
dc.description.abstractVarious BRAF kinase inhibitors were developed to treat cancers carrying the BRAFV600E mutation. First-generation BRAF inhibitors could lead to paradoxical activation of the MAPK pathway, limiting their clinical usefulness. Here, we show the development of two series of BRAFV600E-targeting PROTACs and demonstrate that the exchange of the inhibitor scaffold from vemurafenib to paradox-breaker ligands resulted in BRAFV600E degraders that did not cause paradoxical ERK activation.
dc.languageen
dc.language.isoeng
dc.publisherROYAL SOC CHEMISTRY
dc.rights.urihttp://www.rioxx.net/licenses/all-rights-reserved
dc.titleEncoding BRAF inhibitor functions in protein degraders.
dc.typeJournal Article
dcterms.dateAccepted2022-05-05
rioxxterms.versionAM
rioxxterms.versionofrecord10.1039/d2md00064d
dc.relation.isPartOfRSC Medicinal Chemistry
pubs.notesNot 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/Medicinal Chemistry 2
pubs.publication-statusPublished online
pubs.embargo.termsNot known
icr.researchteamMedicinal Chemistry 2
dc.contributor.icrauthorRossanese, Olivia
dc.contributor.icrauthorCollins, Ian


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