Target intelligence / Profile preview

Potassium voltage-gated channel subfamily H member 1 (KCNH1) (KCNH1)

Target
KCNH1
Molecular classification
Ion channel, Voltage-gated potassium channel
01

Overview

Potassium voltage-gated channel subfamily H member 1 (Kv10.1), also known as EAG1, is a voltage-gated potassium channel that plays a significant role in the regulation of the cell cycle and proliferation (Pardo & Stühmer, 2014). While its physiological expression is largely restricted to the central nervous system, it is frequently overexpressed in a wide variety of human cancers, including breast, lung, and prostate carcinomas (Weber et al., 2006). This restricted expression pattern makes it an attractive target for cancer therapy, as targeting the channel or its mRNA may minimize peripheral side effects (Downie et al., 2008). In oncogenesis, Kv10.1 contributes to tumor progression by modulating membrane potential and intracellular signaling pathways that favor cell survival and migration (Borowiec et al., 2007). Therapeutic strategies include small-molecule inhibitors, monoclonal antibodies, and RNA interference (siRNA) specifically targeting the Kv10.1 mRNA to downregulate protein expression (Gómez-Varela et al., 2007). However, drug development must carefully manage potential cross-reactivity with the closely related hERG channel (Kv11.1) to avoid cardiotoxicity (Sánchez-Alonso et al., 2010).

Other names
Kv10.1EAG1Ether-a-go-go 1hEAG1KCNH1 mRNA
02

Mechanism of action

Potassium channel inhibition and RNA interference-mediated gene silencing

03

Biological functions

Cell cycle regulationCell proliferationPotassium ion transportSignal transduction
04

Disease associations

CancerTemple-Baraitser syndromeZimmermann-Laband syndrome
05

Safety considerations

Cardiac arrhythmia due to hERG cross-reactivityPotential central nervous system side effects
06

Interacting drugs

Astemizole

4 more in the full profile.

07

Biomarkers

KCNH1 mRNA expression levelsKv10.1 protein surface expression

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