Design and synthesis of glyco-peptides as anti-cancer agents targeting thrombin-protease activated receptor-1 interaction. Issue 43 (24th April 2020)

• Record Type: Journal Article
• Authors: Chang, Yu-Hsuan; Wu, Jen-Chine; Yu, Hui-Ming; Hsu, Hua-Ting; Wu, Ying-Ta; Yu, Alice Lin-Tsing; Yu, Cheng-Der Tony; Wong, Chi-Huey
• Is Part Of: Chemical communications. Volume 56:Issue 43(2020)
• Page Start: 5827
• Page End: 5830
• Publication Date: 2020-04-24
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d0cc01240h
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Anti-cancer glyco-peptides inhibit the thrombin-protease activated receptor-1 interaction in exosite I without affecting the active-site mediated coagulation activity. Abstract : Thrombin activates protease-activated receptor-1 (PAR-1) through binding to exosite I and the active site to promote tumor growth. We have developed a new class of anti-cancer glyco-peptides to target exosite I selectively without affecting the active-site-mediated coagulation activity and showed the importance of glycans for the stability and anti-cancer activity of the glyco-peptides.