Browsing by Author "Chan, LY"
Now showing 1 - 1 of 1
Results Per Page
Sort Options
- ItemCyclization of the antimicrobial peptide gomesin with native chemical ligation: influences on stability and bioactivity(Wiley-V C H Verlag, 2013-03-18) Chan, LY; Zhang, VM; Huang, YH; Waters, NC; Bansal, PS; Craik, DJ; Daly, NLGomesin is an 18-residue peptide originally isolated from the hemocytes of the Brazilian spider Acanthoscurria gomesiana. A broad spectrum of bioactivities have been attributed to gomesin, including in vivo and in vitro cytotoxicity against tumour cells, antimicrobial, antifungal, anti-Leishmania and antimalarial effects. Given the potential therapeutic applications of gomesin, it was of interest to determine if an engineered version with a cyclic backbone has improved stability and bioactivity. Cyclization has been shown to confer enhanced stability and activity to a range of bioactive peptides and, in the case of a cone snail venom peptide, confer oral activity in a pain model. The current study demonstrates that cyclization improves the in vitro stability of gomesin over a 24 hour time period and enhances cytotoxicity against a cancer cell line without being toxic to a noncancerous cell line. In addition, antimalarial activity is enhanced upon cyclization. These findings provide additional insight into the influences of backbone cyclization on the therapeutic potential of peptides. © 2013, Wiley-VCH Verlag.