Cyclization of the antimicrobial peptide gomesin with native chemical ligation: influences on stability and bioactivity

Simple item page
dc.contributor.authorChan, LYen_AU
dc.contributor.authorZhang, VMen_AU
dc.contributor.authorHuang, YHen_AU
dc.contributor.authorWaters, NCen_AU
dc.contributor.authorBansal, PSen_AU
dc.contributor.authorCraik, DJen_AU
dc.contributor.authorDaly, NLen_AU
dc.date.accessioned2013-11-19T04:48:54Zen_AU
dc.date.available2013-11-19T04:48:54Zen_AU
dc.date.issued2013-03-18en_AU
dc.date.statistics2013-11-19en_AU
dc.description.abstractGomesin 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.en_AU
dc.identifier.citationChan, L. Y., Zhang, V. M., Huang, Y. H., Waters, N. C., Bansal, P. S., Craik, D. J., & Daly, N. L. (2013). Cyclization of the antimicrobial peptide gomesin with native chemical ligation: influences on stability and bioactivity. ChemBioChem, 14 (5), 617-624. doi:10.1002/cbic.201300034en_AU
dc.identifier.govdoc5157en_AU
dc.identifier.issn1439-4227en_AU
dc.identifier.issue5en_AU
dc.identifier.journaltitleChemBioChemen_AU
dc.identifier.pagination617-624en_AU
dc.identifier.urihttp://dx.doi.org/10.1002/cbic.201300034en_AU
dc.identifier.urihttp://apo.ansto.gov.au/dspace/handle/10238/4956en_AU
dc.identifier.volume14en_AU
dc.language.isoenen_AU
dc.publisherWiley-V C H Verlagen_AU
dc.subjectPeptidesen_AU
dc.subjectAntimitotic drugsen_AU
dc.subjectSpidersen_AU
dc.subjectIn vivoen_AU
dc.subjectIn vitroen_AU
dc.subjectNeoplasmsen_AU
dc.titleCyclization of the antimicrobial peptide gomesin with native chemical ligation: influences on stability and bioactivityen_AU
dc.typeJournal Articleen_AU
Files
License bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
license.txt
Size:
1.71 KB
Format:
Item-specific license agreed upon to submission
Description:
Download
Collections
Journal Articles