Bridged α-helix mimetic small molecules

Literature Information

Publication Date 2019-10-10
DOI 10.1039/C9CC03627J
Impact Factor 6.222
Authors

Yeongju Lee, Haeri Im, Sanket Das, Misook Oh, Ji Hoon Lee, Sihyun Ham, Hyun-Suk Lim


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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.

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