Population
Kv7.1/KCNE1 channels (in vitro/preclinical model)
Design
Preclinical
Key result
The adamantane compound AC-1 potently inhibits Kv7.1/KCNE1 channels with an IC50 of 78.4 nM by binding to fenestrations that form only when KCNE1 accessory subunits are bound to Kv7.1 channels.
Authors
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Offers selective probe for IKs research; leaves open therapeutic translation in channelopathies.
Effect estimate: IC50 78.4 nM
The discovery that KCNE1 induces fenestrations in Kv7.1 channels provides a structural basis for developing highly subtype-specific ion channel inhibitors.
Wrobel et al. (2016) studied Kv7.1/KCNE1 channel function. AC-1 (JNJ303) vs. Control (homomeric Kv7.1 or no drug) was evaluated on Half-maximum inhibitory concentration (IC50) for Kv7.1/KCNE1 currents (IC50 78.4 nM). The adamantane compound AC-1 potently inhibits Kv7.1/KCNE1 channels with an IC50 of 78.4 nM by binding to fenestrations that form only when KCNE1 accessory subunits are bound to Kv7.1 channels.