Authors: Wiedemann, Bianca
Kamps, Dominic
Depta, Laura
Weisner, Jörn
Cvetreznik, Jana
Tomassi, Stefano
Gentz, Sascha
Hoffmann, Jan-Erik
Müller, Matthias P.
Koch, Oliver
Dehmelt, Leif
Rauh, Daniel
Title: Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions
Language (ISO): en
Abstract: Misregulation 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.
Subject Headings: Fluorescence polarization
DNA electrophoresis
Electrophoretic mobility shift assay
HeLa cells
Nucleic acids
Peptide synthesis
Transcription factors
Subject Headings (RSWK): DNA
Issue Date: 2022-06-22
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Appears in Collections:Medizinische Chemie und Chemische Biologie

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