Biomedicines, Volume 6, Issue 3
2018 September - 21 articles
Cover Story: Spider venoms are rich in insecticidal peptides, but as venoms are usually injected, there has been no evolutionary pressure to produce venom peptides with oral activity. Nevertheless, some orally active venom peptides were recently reported, although their oral activity was significantly lower than by injection. Therefore, we systematically evaluated several chemical strategies to increase the oral potency of the insecticidal spider-venom peptide ω-HXTX-Hv1a (Hv1a). N- to C-terminal cyclisation and replacement of disulfide by diselenide bonds failed to improve oral activity. Cyclization of Hv1a dramatically reduced the translocation of Hv1a across the insect midgut, highlighting the importance of bioavailability for oral activity. Hadronyche versuta photo courtesy of Mike Gray (Australian Museum) View the paper here.
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Biomedicines - ISSN 2227-9059