Synthesis of proline analogues as potent and selective cathepsin S inhibitors

  • Kim, Mira; 
  • Jeon, Jiyoung; 
  • Song, Jiyeon; 
  • Suh, Kwee Hyun; 
  • Kim, Young Hoon; 
  • ... Min, Kyung Hoon; 
  • 외 1명
Citations

WEB OF SCIENCE

19
Citations

SCOPUS

18

초록

Cathepsin S is a potential target of autoimmune disease. A series of proline derived compounds were synthesized and evaluated as cathepsin S inhibitors. We discovered potent cathepsin S inhibitors through structure-activity relationship studies of proline analogues. In particular, compound 19-(S) showed promising in vitro/vivo pharmacological activities and properties as a selective cathepsin S inhibitor.

키워드

Cathepsin S; Proline analogues; Small molecules; MHC CLASS-II; ANTIGEN PRESENTATION; CYSTEINE CATHEPSINS; PROTEASE INHIBITOR; INDUCED ARTHRITIS; DESIGN; ANGIOGENESIS; DISEASE; ROLES; MICE
제목
Synthesis of proline analogues as potent and selective cathepsin S inhibitors
저자
Kim, Mira; Jeon, Jiyoung; Song, Jiyeon; Suh, Kwee Hyun; Kim, Young Hoon; Min, Kyung Hoon; Lee, Kwang-Ok
DOI
10.1016/j.bmcl.2013.04.023
발행일
2013-06
유형
Article
저널명
Bioorganic & Medicinal Chemistry Letters
권
23
호
11
페이지
3140 ~ 3144