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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 |
Issue Date: | 29-Apr-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/123456789/2956 |
Appears in Collections: | Department of Chemistry |
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