Bridged α-helix mimetic small molecules
Literature Information
Yeongju Lee, Haeri Im, Sanket Das, Misook Oh, Ji Hoon Lee, Sihyun Ham, Hyun-Suk Lim
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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