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Ztz240 activates KCNQ2. 5 / 5
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"Here , we report cryo-electron microscopy ( cryo-EM ) structures of the human KCNQ2 determined in apo state and in complex with two activators , ztz240 or retigabine , which activate KCNQ2 through different mechanisms ."
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"We found that, without any adjustment of parameters produced by fitting the concentration response data of ztz240 potentiating the WT KCNQ2 channel, the concentration response curve of ztz240 activating the WT-F137A heteromeric channel predicted by our statistical thermodynamic model is in good agreement with the experimental data determined here in parallel."
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"In the present study, we have demonstrated that our model provides an excellent fit to the concentration response data of ztz240 activating the KCNQ2 channel; the fitting result is much better than the fit by the widely used Hill equation."
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"Before that, we obtained a set of concentration response data for ztz240 potentiating KCNQ2 by determining the outward current (I/I 0 values) at different concentrations of ztz240."
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"Ztz240, another KCNQ activator that is distinct from retigabine and ZnPy, potentiates KCNQ2 and KCNQ4 but does not affect KCNQ1 and KCNQ3."
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