Isolation and characterization of a novel conus peptide with apparent antinociceptive activity

J Biol Chem. 2000 Oct 20;275(42):32391-7. doi: 10.1074/jbc.M003619200.

Abstract

Cone snails are tropical marine mollusks that envenomate prey with a complex mixture of neuropharmacologically active compounds. We report the discovery and biochemical characterization of a structurally unique peptide isolated from the venom of Conus marmoreus. The new peptide, mr10a, potently increased withdrawal latency in a hot plate assay (a test of analgesia) at intrathecal doses that do not produce motor impairment as measured by rotarod test. The sequence of mr10a is NGVCCGYKLCHOC, where O is 4-trans-hydroxyproline. This sequence is highly divergent from all other known conotoxins. Analysis of a cDNA clone encoding the toxin, however, indicates that it is a member of the recently described T-superfamily. Total chemical synthesis of the three possible disulfide arrangements of mr10a was achieved, and elution studies indicate that the native form has a disulfide connectivity of Cys1-Cys4 and Cys2-Cys3. This disulfide linkage is unprecedented among conotoxins and defines a new family of Conus peptides.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Analgesics / chemistry
  • Analgesics / pharmacology*
  • Animals
  • Conotoxins / chemistry*
  • Conotoxins / pharmacology*
  • Electric Stimulation
  • Hot Temperature
  • In Vitro Techniques
  • Male
  • Mice
  • Molecular Sequence Data
  • Oocytes / drug effects
  • Oocytes / physiology
  • Pain / physiopathology*
  • Pain / prevention & control
  • Peptide Fragments / chemistry
  • Peptide Fragments / pharmacology*
  • Protein Subunits
  • Rana pipiens
  • Receptors, Nicotinic / drug effects
  • Receptors, Nicotinic / genetics
  • Receptors, Nicotinic / physiology*
  • Recombinant Proteins / drug effects
  • Sequence Alignment
  • Sequence Homology, Amino Acid
  • Spinal Nerves / drug effects
  • Spinal Nerves / physiology*
  • Xenopus laevis

Substances

  • Analgesics
  • Conotoxins
  • Peptide Fragments
  • Protein Subunits
  • Receptors, Nicotinic
  • Recombinant Proteins