Co-expression of NaVβ subunits alters the kinetics of inhibition of voltage-gated sodium channels by pore-blocking μ-conotoxins

Autor: Doju Yoshikami, Baldomero M. Olivera, Jean Rivier, Joanna Gajewiak, Grzegorz Bulaj, Layla Azam, Michael J. Wilson, Min Min Zhang
Rok vydání: 2013
Předmět:
Zdroj: British Journal of Pharmacology. 168:1597-1610
ISSN: 0007-1188
DOI: 10.1111/bph.12051
Popis: Background and Purpose Voltage-gated sodium channels (VGSCs) are assembled from two classes of subunits, a pore-bearing α-subunit (NaV1) and one or two accessory β-subunits (NaVβs). Neurons in mammals can express one or more of seven isoforms of NaV1 and one or more of four isoforms of NaVβ. The peptide μ-conotoxins, like the guanidinium alkaloids tetrodotoxin (TTX) and saxitoxin (STX), inhibit VGSCs by blocking the pore in NaV1. Hitherto, the effects of NaVβ-subunit co-expression on the activity of these toxins have not been comprehensively assessed.
Databáze: OpenAIRE
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