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초록
Herein, we report a strategy for generating conformationally restricted alpha-helix mimetic small molecules by introducing covalent bridges that limit rotation about the central axis of alpha-helix mimetics. We demonstrate that the bridged alpha-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.
키워드
INHIBITION; LIBRARIES; MIMICS; MCL-1
- 제목
- Bridged alpha-helix mimetic small molecules
- 저자
- Lee, Yeongju; Im, Haeri; Das, Sanket; Oh, Misook; Lee, Ji Hoon; Ham, Sihyun; Lim, Hyun-Suk
- 발행일
- 2019-11
- 유형
- Article
- 권
- 55
- 호
- 88
- 페이지
- 13311 ~ 13314