Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors
Document Type
Article
Date of Original Version
6-1-2006
Abstract
A series of peptide analogues of Ac-CIYKYY (1) were synthesized by functional group modifications in peptide side chains or by introducing conformational constraints, to improve the inhibitory potency against active Src kinase. Ac-CIYKF(4-NO2)Y (2, IC50 = 0.53 μM) and conformationally constrained peptide 31 (IC50 = 0.28 μM) exhibited 750- and 1400-fold higher inhibitory activities, respectively, versus that of 1 (IC50 = 400 μM). Compound 2 exhibited a partial competitive inhibition pattern against ATP. © 2006 American Chemical Society.
Publication Title, e.g., Journal
Journal of Medicinal Chemistry
Volume
49
Issue
11
Citation/Publisher Attribution
Kumar, Anil, Guofeng Ye, Yuehao Wang, Xiaofeng Lin, Gongqin Sun, and Keykavous Parang. "Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors." Journal of Medicinal Chemistry 49, 11 (2006): 3395-3401. doi: 10.1021/jm060334k.