Cyclic Peptides as Protein Kinase Inhibitors: Structure-Activity Relationship and Molecular Modeling.

ABSTRACT: Under-expression or overexpression of protein kinases has been shown to be associated with unregulated cell signal transduction in cancer cells. Therefore, there is major interest in designing protein kinase inhibitors as anticancer agents. We have previously reported [WR]₅, a peptide containing alternative arginine (R) and tryptophan (W) residues as a non-competitive c-Src tyrosine kinase inhibitor. A number of larger cyclic peptides containing alternative hydrophobic and positively charged residues [WR]_x (x = 6-9) and hybrid cyclic-linear peptides, [R₆K]W₆ and [R₅K]W₇, containing R and W residues were evaluated for their protein kinase inhibitory potency. Among all the peptides, cyclic peptide [WR]₉

SUBMITTER: Sanner MF 

PROVIDER: S-EPMC8238896 | biostudies-literature | 2021 Jun

REPOSITORIES: biostudies-literature