Many analogues maintain the same level of non-selective cytotoxicity of TG and three analogues are completely non-toxic. We showed that the cytotoxicity is tuneable by single amino-acids substitutions. In the present work, we studied thirteen TG analogues, adopting a multidisciplinary approach. Trichogin GA IV (TG) is a short peptaibol displaying antimicrobial and cytotoxic activity. 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. Peptaibols are peculiar peptides produced by fungi as weapons against other microorganisms.
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