Bioactive Mimetics of Conotoxins and other Venom Peptides

Toxins (Basel). 2015 Oct 16;7(10):4175-98. doi: 10.3390/toxins7104175.

Abstract

Ziconotide (Prialt®), a synthetic version of the peptide ω-conotoxin MVIIA found in the venom of a fish-hunting marine cone snail Conus magnus, is one of very few drugs effective in the treatment of intractable chronic pain. However, its intrathecal mode of delivery and narrow therapeutic window cause complications for patients. This review will summarize progress in the development of small molecule, non-peptidic mimics of Conotoxins and a small number of other venom peptides. This will include a description of how some of the initially designed mimics have been modified to improve their drug-like properties.

Keywords: Cav2.2; N-type calcium channel; conotoxins; peptidomimetics; toxins; venom peptides.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Calcium Channel Blockers / chemistry*
  • Calcium Channel Blockers / pharmacology
  • Calcium Channels, N-Type / metabolism
  • Cell Line, Tumor
  • Humans
  • Models, Molecular
  • Molecular Sequence Data
  • Molecular Structure
  • Mollusk Venoms / chemistry*
  • Mollusk Venoms / pharmacology
  • Patch-Clamp Techniques
  • Peptidomimetics / chemistry*
  • Peptidomimetics / pharmacology
  • omega-Conotoxins / chemistry*
  • omega-Conotoxins / pharmacology

Substances

  • Calcium Channel Blockers
  • Calcium Channels, N-Type
  • Mollusk Venoms
  • Peptidomimetics
  • omega-Conotoxins
  • Conus magus toxin
  • ziconotide