Biochemical characterization and nuclear magnetic resonance structure of novel alpha-conotoxins isolated from the venom of Conus consors

Biochemistry. 1999 May 11;38(19):6317-26. doi: 10.1021/bi982817z.

Abstract

Two novel alpha-conotoxins were purified and characterized from the venom of the fish-hunting cone snail Conus consors. These peptides were identified by screening HPLC fractions of the crude venom and by binding experiments with Torpedo nicotinic acetylcholine receptor. The toxins named alpha-CnIA and alpha-CnIB exhibited sequences of 14 and 12 amino acids, respectively. The alpha-CnIA represents the main alpha-conotoxin contained in the venom, whereas alpha-CnIB is present in a relatively small amount. Chemical synthesis of alpha-CnIA was carried out using the Fmoc methodology by selective disulfide bond formation. The biological activity of the toxin was assessed in fish and mice. The alpha-CnIA inhibited the fixation of iodinated alpha-bungarotoxin to Torpedo nicotinic acetylcholine receptors with an IC50 of 0.19 microM which can be compared to the IC50 of 0.31 microM found for the previously characterized alpha-MI isolated from the piscivorous Conus magus. The synthetic alpha-CnIA blocked spontaneous and evoked synaptic potentials in frog and mouse isolated neuromuscular preparations at sub-micromolar concentrations. Solution NMR of this toxin indicated a conformational heterogeneity with the existence of different conformers in solution, at slow and intermediate exchange rates relative to the NMR chemical shift time scale, similar to that reported for alpha-GI and alpha-MI. NMR structures were calculated for the major NMR signals representing more than 80% of the population at 5 degrees C.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Biological Assay
  • Bungarotoxins / pharmacology
  • Conotoxins*
  • Iodine Radioisotopes
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Sequence Data
  • Mollusca / chemistry
  • Mollusk Venoms / chemistry*
  • Nicotinic Antagonists / pharmacology
  • Oligopeptides / chemistry*
  • Oligopeptides / isolation & purification
  • Oligopeptides / pharmacology
  • Peptides / chemistry*
  • Peptides / isolation & purification
  • Peptides / pharmacology
  • Peptides, Cyclic / chemistry
  • Protein Conformation
  • Receptors, Nicotinic / metabolism
  • Sequence Homology, Amino Acid

Substances

  • Bungarotoxins
  • Conotoxins
  • Iodine Radioisotopes
  • Mollusk Venoms
  • Nicotinic Antagonists
  • Oligopeptides
  • Peptides
  • Peptides, Cyclic
  • Receptors, Nicotinic
  • alpha-conotoxin IA
  • alpha-conotoxin IB
  • conotoxin GI

Associated data

  • PDB/1B45