Cargando…

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

Selective blockers of the N-type voltage-sensitive calcium (Ca(V)) channels are useful in the management of severe chronic pain. Here, the structure and function characteristics of a novel N-type Ca(V) channel blocker, SO-3, are reviewed. SO-3 is a 25- amino acid conopeptide originally derived from...

Descripción completa

Detalles Bibliográficos
Autores principales: Wen, Lei, Yang, Sheng, Zhou, Wenxia, Zhang, Yongxiang, Huang, Peitang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2006
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3663411/
_version_ 1782270991449194496
author Wen, Lei
Yang, Sheng
Zhou, Wenxia
Zhang, Yongxiang
Huang, Peitang
author_facet Wen, Lei
Yang, Sheng
Zhou, Wenxia
Zhang, Yongxiang
Huang, Peitang
author_sort Wen, Lei
collection PubMed
description Selective blockers of the N-type voltage-sensitive calcium (Ca(V)) channels are useful in the management of severe chronic pain. Here, the structure and function characteristics of a novel N-type Ca(V) 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 Ca(V) 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 Ca(V) 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 Ca(V) channels.
format Online
Article
Text
id pubmed-3663411
institution National Center for Biotechnology Information
language English
publishDate 2006
publisher Molecular Diversity Preservation International (MDPI)
record_format MEDLINE/PubMed
spelling pubmed-36634112013-05-28 New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels Wen, Lei Yang, Sheng Zhou, Wenxia Zhang, Yongxiang Huang, Peitang Mar Drugs Review Selective blockers of the N-type voltage-sensitive calcium (Ca(V)) channels are useful in the management of severe chronic pain. Here, the structure and function characteristics of a novel N-type Ca(V) 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 Ca(V) 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 Ca(V) 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 Ca(V) channels. Molecular Diversity Preservation International (MDPI) 2006-04-06 /pmc/articles/PMC3663411/ Text en © 2006 by MDPI Reproduction is permitted for noncommercial purposes.
spellingShingle Review
Wen, Lei
Yang, Sheng
Zhou, Wenxia
Zhang, Yongxiang
Huang, Peitang
New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels
title New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels
title_full New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels
title_fullStr New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels
title_full_unstemmed New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels
title_short New Conotoxin SO-3 Targeting N-type Voltage-Sensitive Calcium Channels
title_sort new conotoxin so-3 targeting n-type voltage-sensitive calcium channels
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3663411/
work_keys_str_mv AT wenlei newconotoxinso3targetingntypevoltagesensitivecalciumchannels
AT yangsheng newconotoxinso3targetingntypevoltagesensitivecalciumchannels
AT zhouwenxia newconotoxinso3targetingntypevoltagesensitivecalciumchannels
AT zhangyongxiang newconotoxinso3targetingntypevoltagesensitivecalciumchannels
AT huangpeitang newconotoxinso3targetingntypevoltagesensitivecalciumchannels