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ACS Chem Biol. 2007 Jul 20;2(7):457-68.

Chemical modification of conotoxins to improve stability and activity.

Author information

1
Institute for Molecular Bioscience, The University of Queensland, Brisbane, Australia.

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 conopeptides. They enhance the versatility of these peptides as tools in neuroscience and as drug leads.

PMID:
17649970
DOI:
10.1021/cb700091j
[Indexed for MEDLINE]

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