Chemical modification of conotoxins to improve stability and activity

Authors

David J. Craik, University of Queensland
David J. Adams, University of QueenslandFollow

RIS ID

105691

Publication Details

Craik, D. J. & Adams, D. J. (2007). Chemical modification of conotoxins to improve stability and activity. ACS Chemical Biology, 2 (7), 457-468.

Abstract

Conotoxins are small disulfide-rich peptides from the venom of cone snails. Along with other conopeptides, they target a wide range of membrane receptors, ion channels, and transporters, and because of their high potency and selectivity for defined subtypes of these receptors, they have attracted a great deal of attention recently as leads in drug development. However, like most peptides, conopeptides potentially suffer from the disadvantages of poor absorption, poor stability, or short biological half-lives. Recently, various chemical approaches, including residue substitutions, backbone cyclization, and disulfide-bridge modification, have been reported to increase the stability of conopeptides. These manufactured interventions add to the array of post-translational modifications that occur naturally in conopeplides. They enhance the versatility of these peptides as tools in neuroscience and as drug leads.