A cell-active cyclic peptide targeting the Nrf2/Keap1 protein–protein interaction

Chem. Sci., 2023, 14,10800-10805
DOI: 10.1039/D3SC04083F, Edge Article
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Creative Commons Licence  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Jessica Iegre, Sona Krajcovicova, Anders Gunnarsson, Lisa Wissler, Helena Käck, Anna Luchniak, Stefan Tångefjord, Frank Narjes, David R. Spring
Application of DVP stapling methodology to efficiently develop Nrf2 peptides with nM activity in enzymatic assays, submicromolar activity in cells and non-cytotoxicity, characterised by high resolution X-ray co-crystallography.
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