AGAP, a new recombinant neurotoxic polypeptide, targets the voltage-gated calcium channels in rat small diameter DRG neurons.
Biochem Biophys Res Commun
; 452(1): 60-5, 2014 Sep 12.
Article
em En
| MEDLINE
| ID: mdl-25148943
ABSTRACT
A previous study showed that antitumor-analgesic peptide (AGAP), a novel recombinant polypeptide, which had been expressed in Escherichia coli, exhibits analgesic and antitumor effects in mice. In the present study, we investigated the underlying analgesic mechanism of AGAP. The effect of AGAP on voltage-gated calcium channels (VGCCs) was assessed in acutely isolated rat dorsal root ganglia (DRG) neurons using the whole-cell patch clamp technique. The results showed that AGAP potently inhibited VGCCs, especially high-voltage activated (HVA) calcium channels. AGAP inhibited HVA and T-type calcium currents in a dose-dependent manner, but had no significant effect on their dynamic functions in rat small-diameter DRG neurons. AGAP inhibited N- and L-type calcium currents at 78.2% and 57.3%, respectively. Thus, the present study demonstrates that AGAP affects calcium currents through the inhibition of N-, L- and T-type channels in DRG neurons, explaining the potential mechanisms of antinociception.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Venenos de Escorpião
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Ativação do Canal Iônico
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Canais de Cálcio Tipo T
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Gânglios Espinais
Limite:
Animals
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article