Related Experiment Video
Updated: Jun 18, 2026
10:07
High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
Voltage-gated potassium channels as therapeutic targets
Heike Wulff1, Neil A Castle, Luis A Pardo
1Department of Pharmacology, University of California, Davis, 451 Health Sciences Drive, GBSF Room 3502, Davis, California 95616, USA. hwulff@ucdavis.edu
Nature Reviews. Drug Discovery
|December 2, 2009
Summary
Voltage-gated K(+) channels (K(V)) are crucial for numerous physiological functions. This review explores drug development strategies targeting K(V) channels for various diseases.
Area of Science:
- Pharmacology
- Molecular Biology
- Physiology
Background:
- The human genome encodes 40 types of voltage-gated potassium channels (K(V)).
- K(V) channels play vital roles in neuronal and cardiac repolarization, calcium signaling, cell volume, and proliferation.
- Dysfunction of K(V) channels is implicated in diseases like cancer, autoimmune disorders, and neurological conditions.
Purpose of the Study:
- To review pharmacological strategies for targeting K(V) channels.
- To highlight recent advancements in drug development for K(V) channel-related diseases.
Main Methods:
- Discussion of various targeting agents including venom peptides, antibodies, and small molecules.
- Review of preclinical and clinical progress for specific K(V) channel subfamilies.
Main Results:
- K(V) channels represent significant therapeutic targets for a range of diseases.
- Pharmacological targeting of K(V) channels shows promise for drug development.
Conclusions:
- Targeting K(V) channels offers a promising avenue for novel therapeutics.
- Continued research into K(V) channel modulation is essential for treating complex diseases.
Related Concept Videos
01:26Voltage-gated Ion Channels
Voltage-gated ion channels are transmembrane proteins that open and close in response to changes in the membrane potential. They are present on the membranes of all electrically excitable cells such as neurons, heart, and muscle cells.
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several types of...
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several types of...
01:26Voltage-gated Ion Channels
Voltage-gated ion channels are transmembrane proteins that open and close in response to changes in the membrane potential. They are present on the membranes of all electrically excitable cells such as neurons, heart, and muscle cells.
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several types of...
Generally, all voltage-gated ion channels have a 'voltage-sensing domain' that spans the lipid bilayer. The charged residues in the sensor move in response to the membrane potential changes that open the channel allowing ions movement. There are several types of...
01:24Non-gated Ion Channels
Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
01:24Non-gated Ion Channels
Ion channels are specialized proteins on the plasma membrane that allow charged ions to pass down their electrochemical gradient. Their main function is to maintain the membrane potential which is critical for cell viability. These channels are either gated or non-gated and can transport more than a thousand ions within milliseconds for the cellular event to occur.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
Compared to the gated ion channels, the non-gated channels, also known as leakage or passive channels, have no gating mechanism.
01:20Antiepileptic Drugs: Potassium Channel Activators
Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
Ezogabine has gained approval as an adjunctive treatment...
01:12Antiarrhythmic Drugs: Class III Agents as Potassium Channel Blockers
Class III antiarrhythmic drugs are a group of medications that can prolong action potentials in the heart. They achieve this by blocking potassium channels or enhancing inward currents from sodium channels. However, these drugs have a unique property of "reverse use-dependence," which is most pronounced at slower heart rates and can lead to torsades de pointes—a specific type of arrhythmia. However, it is essential to note that excessive QT interval prolongation—a measure of the heart's...