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Mar. Drugs 2006, 4(3), 215-227; https://doi.org/10.3390/md403215

New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels

1
Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China
2
School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, China
3
Beijing Institute of Biotechnology, Beijing 100071, China
*
Author to whom correspondence should be addressed.
Received: 10 March 2006 / Accepted: 30 March 2006 / Published: 6 April 2006
(This article belongs to the Special Issue Marine Drugs and Ion Channels)
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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. View Full-Text
Keywords: ω-conotoxins; SO-3; MVIIA; voltage-sensitive calcium channels; N-type calcium channel blockers; pain ω-conotoxins; SO-3; MVIIA; voltage-sensitive calcium channels; N-type calcium channel blockers; pain
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Wen, L.; Yang, S.; Zhou, W.; Zhang, Y.; Huang, P. New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels. Mar. Drugs 2006, 4, 215-227.

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