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Potassium channel subfamily V member 2 (Kv2.1) (Kv2.1)

Target
Kv2.1
Molecular classification
Ion channel, Voltage-gated potassium channel, Membrane protein
01

Overview

Potassium channel subfamily V member 2 (Kv2.1) is a voltage-gated potassium channel that forms tetramers in the plasma membrane, concentrated in clusters or as single, diffusely distributed channels. It is widely expressed in the mammalian central nervous system, especially in hippocampal and cortical neurons. Kv2.1 plays a major role in generating the delayed rectifier K+ current responsible for repolarizing the membrane after action potentials and regulating neuronal excitability during periods of high-frequency firing. The channel also contributes to processes including apoptosis, cell cycle progression, and membrane protein trafficking. Dysregulation and mutations in Kv2.1 have been linked to cancer progression, particularly in highly metastatic prostate cancer, and to genetic epileptic encephalopathies. Kv2.1 is a therapeutic target for pharmacological inhibition, with known blockers such as stromatoxin-1, RY785, and experimental tools like KC antibody. Its clustering, trafficking, and conductance are tightly regulated by cytoplasmic signaling pathways and cytoskeletal elements.

Other names
Voltage-gated potassium channel Kv2.1KCNB1delayed rectifier K+ channelPotassium channel subfamily V member 2
02

Mechanism of action

Inhibition of Kv2.1 by peptide toxins or small molecule ligands blocks potassium current, affecting cell membrane polarization and cellular excitability. Facilitated pore closure (RY785). Blocking of channel function via antibody interaction (KC antibody).

03

Biological functions

Regulation of membrane potentialAction potential repolarizationControl of neuronal excitabilityApoptosisCell cycle regulationCalcium ion entry modulationMembrane protein trafficking
04

Disease associations

Cancer (e.g., prostate cancer)Epileptic encephalopathiesNeurodegenerative disease (implied by role in apoptosis and neuronal excitability)Other (potential involvement in ischemia and hypoxia responses)
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Safety considerations

Off-target effects on neuronal excitability leading to seizures or neurotoxicityPotential impacts on apoptosis in non-target tissuesDysregulation of membrane potential can lead to arrhythmia or other excitability disorders
06

Interacting drugs

Stromatoxin-1 (ScTx-1)

2 more in the full profile.

07

Biomarkers

Kv2.1 expression in certain cancers (prostate cancer)Kv2.1 mutations in epileptic encephalopathies

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