IndraLab

Statements

Isocyanic acid activates KCNH1-F359L. 5 / 5
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"The homologous mutation in hEAG1 (F359L) also dramatically altered drug action; instead of inhibition, ICA activated F359L hEAG1."
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"Moreover, opposite to WT hEAG1 channels, but similar to WT hERG1, F359L hEAG1 channels were activated by ICA."
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"F359L hEAG1 is activated by ICA."
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"Thus, ICA is an activator of F359L hEAG1 and an inhibitor of F359L and Y464A hEAG1 channels, indicating that Phe359 in S5 is required for ICA to induce open-state inactivation, as well as demonstrating that Tyr464 in S6 is required for the activator effect of ICA on F359L hEAG1 channels."
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"Instead, we found that ICA increased F359L hEAG1 channel currents by 5.4 +/- 0.6-fold at 10 microM (n = 3) without any evident change in kinetics (XREF_FIG)."
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