Please use this identifier to cite or link to this item:
http://dspace.bits-pilani.ac.in:8080/jspui/xmlui/handle/123456789/2950
Title: | Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors |
Authors: | Kumar, Anil |
Keywords: | Chemistry Peptides and proteins Monomers Inhibitors Functional groups |
Issue Date: | 2006 |
Publisher: | ACS |
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. |
URI: | https://pubs.acs.org/doi/10.1021/jm060334k http://dspace.bits-pilani.ac.in:8080/xmlui/handle/123456789/2950 |
Appears in Collections: | Department of Chemistry |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.