Target intelligence / Profile preview

Potassium voltage-gated channel subfamily A (Kv1) (Kv1)

Target
Kv1
Molecular classification
Ion channel, Voltage-gated ion channel, Potassium channel
01

Overview

The Shaker voltage-gated potassium channel is the prototypical member of the Kv channel superfamily, originally identified in Drosophila and represented in humans by the Kv1 (KCNA) family (UniProt: P14625). These channels are essential for regulating cellular excitability by mediating the selective efflux of potassium ions in response to membrane depolarization, which facilitates the repolarization phase of action potentials (StatPearls: NBK563122). The Shaker-IR variant refers to an Inactivation Removed mutant used extensively in research to study pore kinetics without the interference of fast N-type inactivation (PMID: 24828641). In humans, Kv1 channels are critical for axonal conduction in the nervous system and for the activation of effector memory T cells, specifically the Kv1.3 isoform. Mutations in these channels are linked to disorders such as episodic ataxia type 1 and myokymia, while their pharmacological blockade by drugs like dalfampridine is used to improve walking in patients with multiple sclerosis by enhancing conduction in demyelinated axons (PubMed: 20695026).

Other names
Shaker-related potassium channelKCNA familyShaker-IR (Inactivation Removed)Voltage-gated potassium channel subunit Kv1Shaker-type potassium channel
02

Mechanism of action

Blockade of the ion-conducting pore to prevent potassium efflux, thereby prolonging action potentials and enhancing synaptic transmission or modulating immune cell activation.

03

Biological functions

Membrane repolarizationRegulation of action potential durationNeurotransmitter release regulationT-cell activationMaintenance of resting membrane potentialAxonal conduction
04

Disease associations

Episodic ataxia type 1MyokymiaMultiple sclerosisAutoimmune diseaseNeuromyotonia (Isaac's syndrome)Limbic encephalitisHypomagnesemia
05

Safety considerations

Risk of seizures due to increased neuronal excitabilityPotential for cardiac arrhythmiasNarrow therapeutic index for non-selective blockersParesthesia and neurotoxicity
06

Interacting drugs

Dalfampridine

6 more in the full profile.

07

Biomarkers

Anti-voltage-gated potassium channel (VGPC) antibodiesAnti-LGI1 antibodiesAnti-CASPR2 antibodiesKv1.3 expression on effector memory T cells

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