Voltage-gated potassium channel subfamily KQT (Kv7)

Kv7 potassium channels, also known as KCNQ channels, are a family of voltage-gated potassium channels crucial for regulating the electrical activity of various excitable cells, including neurons, cardiac myocytes, and smooth muscle cells. They play a vital role in maintaining the resting membrane potential and controlling cellular excitability by mediating slowly activating, non-inactivating potassium currents, often referred to as M-currents. Dysfunction or mutations in Kv7 channels are implicated in a wide range of diseases, including neurological disorders like epilepsy, neuropathic pain, anxiety, and depression, as well as cardiovascular conditions such as long QT syndrome and cardiac arrhythmias, and even deafness and diabetes. Consequently, Kv7 channels are considered significant therapeutic targets. Drugs targeting these channels primarily act as activators (agonists) to enhance potassium efflux, thereby hyperpolarizing cell membranes and reducing hyperexcitability, or as inhibitors (antagonists) to increase excitability. While some Kv7 modulators like retigabine have been approved for clinical use, safety concerns such as pigmentation changes and liver damage have led to their withdrawal, highlighting the ongoing challenge of developing selective and safe Kv7-targeting therapies.

Other names

Kv7 potassium channelKCNQ potassium channelM-channelVoltage-gated potassium channel

Kv7 channel activators (agonists) enhance potassium efflux, hyperpolarizing the cell membrane and reducing cellular excitability by stabilizing the channel in its open state or shifting its voltage-dependence of activation to more negative voltages. Kv7 channel inhibitors (antagonists) block potassium efflux, leading to depolarization and increased excitability.