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New conotoxin SO-3 targeting N-type voltage-sensitive calcium channels
Wen, L.; Yang, S.; Zhou, W.; Zhang, Y.; Huang, P. (2006). New conotoxin SO-3 targeting N-type voltage-sensitive calcium channels. Mar. Drugs 4(3): 215-227
In: Marine Drugs. Molecular Diversity Preservation International (MDPI): Basel. ISSN 1660-3397, more
Peer reviewed article  

Available in  Authors 

Keywords
    Neurotoxins; Pain; Pain; Marine

Authors  Top 
  • Wen, L.
  • Yang, S.
  • Zhou, W.
  • Zhang, Y.
  • Huang, P.

Abstract
    Selective blockers of the N-type voltage-sensitive calcium (CaV) channels are useful in the management of severe chronic pain. Here, the structure and function characteristics of a novel N-type CaV channel blocker, SO-3, are reviewed. SO-3 is a 25-amino acid conopeptide originally derived from the venom of Conus striatus, and contains the same 4-loop, 6-cysteine framework (C-C-CC-C-C) as O-superfamily conotoxins. The synthetic SO-3 has high analgesic activity similar to ω-conotoxin MVIIA (MVIIA), a selective N-type CaV channel blocker approved in the USA and Europe for the alleviation of persistent pain states. In electrophysiological studies, SO-3 shows more selectivity towards the N-type CaV channels than MVIIA. The dissimilarity between SO-3 and MVIIA in the primary and tertiary structures is further discussed in an attempt to illustrate the difference in selectivity of SO-3 and MVIIA towards N-type CaV channels.

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