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Target intelligence / Profile preview
Potassium voltage-gated channel subfamily H member 8 (KCNH8)
- Target
- KCNH8
- Molecular classification
- Ion channel, Potassium channel, Voltage-gated channel
01
Overview
Potassium voltage-gated channel subfamily H member 8 (KCNH8) encodes a pore-forming alpha subunit of a voltage-gated delayed rectifier potassium channel. These channels mediate outward-rectifying potassium currents with slow activation, no inactivation, and slow deactivation in response to depolarizing membrane potentials. Their activity is critical for regulating neuronal excitability, neurotransmitter release, heart rate, and other physiological processes. KCNH8 is primarily expressed in the central nervous system and is associated with progressive myoclonic epilepsy and potentially with several cancer types. Therapeutic modulation of KCNH8 may be relevant for neurological and oncological diseases, although targeting must consider potential cardiac and neural safety risks[1][2][3][4][5][6]
- Other names
- Kv12.1ELK3Voltage-gated delayed rectifier potassium channel KCNH8Voltage-gated potassium channel subunit Kv12.1Ether-a-go-go-like potassium channel 3Potassium voltage-gated channel, subfamily H (eag-related), member 8hElk-1
02
Mechanism of action
Blockade or modulation of potassium influx/efflux, thus influencing cellular excitability and action potential duration
03
Biological functions
Regulation of neurotransmitter releaseControl of neuronal excitabilityModulation of heart rateInsulin secretionEpithelial electrolyte transportSmooth muscle contractionCell volume regulation
04
Disease associations
Epilepsy (especially Progressive Myoclonic Epilepsy, with or without renal failure)Potential roles in various cancers (based on expression in brain, kidney, liver, breast, etc.)
05
Safety considerations
Risk of cardiac arrhythmia if channel function is disrupted, as seen with other potassium channels (e.g., hERG/KCNH2 family)Potential neuronal side effects (seizure, altered brain excitability) due to impact on action potential repolarization
06
Interacting drugs
Small-molecule blockers (specific drugs targeting KCNH8 are not well-defined; blockers for voltage-gated potassium channels may modulate its activity[2])
07
Biomarkers
Not defined; potential as a biomarker for epilepsy subtypes or cancer based on expression profiles
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