Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions

Simple item page
dc.contributor.authorWiedemann, Bianca
dc.contributor.authorKamps, Dominic
dc.contributor.authorDepta, Laura
dc.contributor.authorWeisner, Jörn
dc.contributor.authorCvetreznik, Jana
dc.contributor.authorTomassi, Stefano
dc.contributor.authorGentz, Sascha
dc.contributor.authorHoffmann, Jan-Erik
dc.contributor.authorMüller, Matthias P.
dc.contributor.authorKoch, Oliver
dc.contributor.authorDehmelt, Leif
dc.contributor.authorRauh, Daniel
dc.date.accessioned2022-07-28T12:16:39Z
dc.date.available2022-07-28T12:16:39Z
dc.date.issued2022-06-22
dc.description.abstractMisregulation and mutations of the transcription factor Nrf2 are involved in the development of a variety of human diseases. In this study, we employed the technology of stapled peptides to address a protein-DNA-complex and designed a set of Nrf2-based derivatives. Varying the length and position of the hydrocarbon staple, we chose the best peptide for further evaluation in both fixed and living cells. Peptide 4 revealed significant enrichment within the nucleus compared to its linear counterpart 5, indicating potent binding to DNA. Our studies suggest that these molecules offer an interesting strategy to target activated Nrf2 in cancer cells.en
dc.identifier.urihttp://hdl.handle.net/2003/41010
dc.identifier.urihttp://dx.doi.org/10.17877/DE290R-22859
dc.language.isoende
dc.relation.ispartofseriesPLOS ONE;17(6)
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectFluorescence polarizationen
dc.subjectDNA electrophoresisen
dc.subjectElectrophoretic mobility shift assayen
dc.subjectHeLa cellsen
dc.subjectNucleic acidsen
dc.subjectPeptide synthesisen
dc.subjectPermeabilityen
dc.subjectTranscription factorsen
dc.subject.ddc570
dc.subject.ddc540
dc.subject.rswkDNAde
dc.subject.rswkElektrophoresede
dc.subject.rswkTranskriptionsfaktorde
dc.titleDesign and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactionsen
dc.typeTextde
dc.type.publicationtypearticlede
dcterms.accessRightsopen access
eldorado.secondarypublicationtruede
eldorado.secondarypublication.primarycitationWiedemann B, Kamps D, Depta L, Weisner J, Cvetreznik J, Tomassi S, et al. (2022) Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions. PLoS ONE 17(6): e0267651. https://doi.org/10.1371/journal.pone.0267651de
eldorado.secondarypublication.primaryidentifierhttps://doi.org/10.1371/journal.pone.0267651de

Files

Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
journal.pone.0267651.pdf
Size:
1.14 MB
Format:
Adobe Portable Document Format
Description:
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
4.85 KB
Format:
Item-specific license agreed upon to submission
Description:
Download

Collections

Medizinische Chemie und Chemische Biologie