dc.contributor.author | Miller, DSJ | |
dc.contributor.author | Voell, SA | |
dc.contributor.author | Sosič, I | |
dc.contributor.author | Proj, M | |
dc.contributor.author | Rossanese, OW | |
dc.contributor.author | Schnakenburg, G | |
dc.contributor.author | Gütschow, M | |
dc.contributor.author | Collins, I | |
dc.contributor.author | Steinebach, C | |
dc.date.accessioned | 2022-05-18T09:58:14Z | |
dc.date.available | 2022-05-18T09:58:14Z | |
dc.date.issued | 2022-06-22 | |
dc.identifier.citation | RSC Medicinal Chemistry | |
dc.identifier.uri | https://repository.icr.ac.uk/handle/internal/5136 | |
dc.identifier.eissn | 2632-8682 | |
dc.identifier.eissn | 2632-8682 | |
dc.identifier.doi | 10.1039/d2md00064d | |
dc.identifier.doi | 10.1039/d2md00064d | |
dc.description.abstract | Various 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.language | en | |
dc.language.iso | eng | |
dc.publisher | ROYAL SOC CHEMISTRY | |
dc.rights.uri | http://www.rioxx.net/licenses/all-rights-reserved | |
dc.title | Encoding BRAF inhibitor functions in protein degraders. | |
dc.type | Journal Article | |
dcterms.dateAccepted | 2022-05-05 | |
rioxxterms.version | AM | |
rioxxterms.versionofrecord | 10.1039/d2md00064d | |
dc.relation.isPartOf | RSC Medicinal Chemistry | |
pubs.notes | Not 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-status | Published online | |
pubs.embargo.terms | Not known | |
icr.researchteam | Medicinal Chemistry 2 | |
dc.contributor.icrauthor | Rossanese, Olivia | |
dc.contributor.icrauthor | Collins, Ian | |