Abstract
We have examined the effects of two DTX homologues, toxin I and toxin K, on Kv1.1, Kv1.2 and Kv1.6 channels expressed in Xenopus oocytes. Toxin I blocked all three channels; in contrast, toxin K was selective for Kv1.1. Both toxins slowed channel activation and inactivation kinetics with 10 nM toxin I approximately doubling activation and inactivation time constants of Kv1.1. For the first time, we have demonstrated the selectivity of a DTX homologue for a single cloned Kv1 channel and suggest that these toxins may sterically hinder the conformational changes that occur during channel gating.
MeSH terms
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Animals
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Brain / drug effects
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Brain / metabolism
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Chromatography, High Pressure Liquid
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Cloning, Molecular
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Elapid Venoms / pharmacology*
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Electrophysiology
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Humans
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Ion Channel Gating
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Kv1.1 Potassium Channel
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Kv1.2 Potassium Channel
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Neurotoxins / pharmacology*
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Oocytes
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Patch-Clamp Techniques
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Peptides / pharmacology*
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Potassium Channel Blockers*
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Potassium Channels / genetics
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Potassium Channels / metabolism
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Potassium Channels, Voltage-Gated*
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Rats
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Xenopus laevis
Substances
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Elapid Venoms
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KCNA1 protein, human
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KCNA2 protein, human
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Kcna2 protein, rat
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Kv1.2 Potassium Channel
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Neurotoxins
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Peptides
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Potassium Channel Blockers
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Potassium Channels
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Potassium Channels, Voltage-Gated
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dendrotoxin K
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Kv1.1 Potassium Channel
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dendrotoxin