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Figure 7.
Summary of ML252 inhibition in the context of Kv7 activator binding sites. Mutagenesis and docking suggest that ML252 binds to a similar site as pore-targeted activators including retigabine and ML213 in both Kv7.2 (cyan) and Kv7.3 (red). This underlies less potent ML252-mediated inhibition when applied together with a pore-targeted activator. VSD-targeted activators ztz-240 and ICA-069673 bind to a distinct site (only present in Kv7.2), and therefore do not prevent ML252 inhibition.
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