The rational search for selective anticancer derivatives of the peptide Trichogin GA IV: a multi-technique biophysical approach.

ABSTRACT: Peptaibols are peculiar peptides produced by fungi as weapons against other microorganisms. Previous studies showed that peptaibols are promising peptide-based drugs because they act against cell membranes rather than a specific target, thus lowering the possibility of the onset of multi-drug resistance, and they possess non-coded α-amino acid residues that confer proteolytic resistance. Trichogin GA IV (TG) is a short peptaibol displaying antimicrobial and cytotoxic activity. In the present work, we studied thirteen TG analogues, adopting a multidisciplinary approach. We showed that the cytotoxicity is tuneable by single amino-acids substitutions. Many analogues maintain the same level of non-selective cytotoxicity of TG and three analogues are completely non-toxic. Two promising lead com

SUBMITTER: Dalzini A 

PROVIDER: S-EPMC4819177 | biostudies-literature | 2016 Apr

REPOSITORIES: biostudies-literature