Unprotected peptide macrocyclization and stapling via a fluorine-thiol displacement reaction
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DOI: 10.1038/s41467-022-27995-5
Abstract: We report the discovery of a facile peptide macrocyclization and stapling strategy based on a fluorine thiol displacement reaction (FTDR), which renders a class of peptide analogues with enhanced stability, affinity, cellular uptake, and inhibition… read more here.
Keywords: displacement reaction; peptide macrocyclization; fluorine thiol; macrocyclization stapling ... See more keywords
Fluorine-Thiol Displacement Stapling on the Disordered α B of pKID Domain Increases Its Helicity and Affinity to KIX
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DOI: 10.1055/a-2409-3840
Abstract: The development of high-affinity ligands specifically targeting intrinsically disordered protein interactions has remained challenging due to the lack of well-defined binding pockets and shallow binding surfaces commonly found at their interfaces. Here, we employed our… read more here.
Keywords: disordered pkid; affinity kix; affinity; thiol displacement ... See more keywords