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Bridged α-helix mimetic small molecules

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Abstract

Herein, we report a strategy for generating conformationally restricted α-helix mimetic small molecules by introducing covalent bridges that limit rotation about the central axis of α-helix mimetics. We demonstrate that the bridged α-helix mimetics have enhanced binding affinity and specificity to the target protein due to the restricted conformation as well as extra interaction of the bridge with the protein surface.

Graphical abstract: Bridged α-helix mimetic small molecules

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Publication details

The article was received on 10 May 2019, accepted on 10 Oct 2019 and first published on 10 Oct 2019


Article type: Communication
DOI: 10.1039/C9CC03627J
Chem. Commun., 2019, Advance Article

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    Bridged α-helix mimetic small molecules

    Y. Lee, H. Im, S. Das, M. Oh, J. H. Lee, S. Ham and H. Lim, Chem. Commun., 2019, Advance Article , DOI: 10.1039/C9CC03627J

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