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Structural Congeners of Izenamides Responsible for Cathepsin D Inhibition: Insights from Synthesis-Derived Elucidation
- Kim, Hyun Su;
- Kong, Hyejin;
- Kim, Taewoo;
- Lim, Changjin;
- Lee, Seungbeom;
- ... Kim, Seok-Ho;
- 외 1명
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1초록
This study aimed to elucidate the structural congeners of natural izenamides A, B, and C (1-3) responsible for cathepsin D (CTSD) inhibition. Structurally modified izenamides were synthesized and biologically evaluated, and their biologically important core structures were identified. We confirmed that the natural statine (Sta) unit (3S,4S)-gamma-amino-beta-hydroxy acid is a requisite core structure of izenamides for inhibition of CTSD, which is closely related to the pathophysiological roles in numerous human diseases. Interestingly, the statine-incorporated izenamide C variant (7) and 18-epi-izenamide B variant (8) exhibited more potent CTSD-inhibitory activities than natural izenamides.
키워드
marine cyanobacteria; izenamides; cathepsin D; linear depsipeptides; statine; DEFICIENT; PEPTIDE; ATROPHY
- 제목
- Structural Congeners of Izenamides Responsible for Cathepsin D Inhibition: Insights from Synthesis-Derived Elucidation
- 저자
- Kim, Hyun Su; Kong, Hyejin; Kim, Taewoo; Lim, Changjin; Lee, Seungbeom; Kim, Seok-Ho; Suh, Young-Ger
- 발행일
- 2023-04-28
- 유형
- Article
- 저널명
- Marine Drugs
- 권
- 21
- 호
- 5
- 언어
- ENG
- 출판사
- MDPI
- 발행국가
- 스위스
- ISSN
- E 1660-3397