Venom-derived peptide inhibitors of voltage-gated potassium channels


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Abstract

Voltage-gated potassium channels play a key role in human physiology and pathology. Reflecting their importance, numerous channelopathies have been characterised that arise from mutations in these channels or from autoimmune attack on the channels. Voltage-gated potassium channels are also the target of a broad range of peptide toxins from venomous organisms, including sea anemones, scorpions, spiders, snakes and cone snails; many of these peptides bind to the channels with high potency and selectivity. In this review we describe the various classes of peptide toxins that block these channels and illustrate the broad range of three-dimensional structures that support channel blockade. The therapeutic opportunities afforded by these peptides are also highlighted.This article is part of the Special Issue entitled ‘Venom-derived Peptides as Pharmacological Tools.’HIGHLIGHTSVoltage-gated potassium channels play key roles in human physiology and pathology.Numerous channelopathies are associated with these channels.Voltage-gated potassium channels are the target of a wide range of peptide toxins.These peptide toxins adopt many different three-dimensional structures.Voltage-gated potassium channels are valuable therapeutic targets.

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