IndraLab

Statements

FOXH1 inhibits SCN5A. 10 / 10
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"LQT3 arises from mutations that disrupt fast inactivation of the cardiac sodium channel SCN5A ( xref )."
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"The EC 50 values of Lqh II, Lqh III, and LqhαIT to remove fast inactivation of hH1 channels are 12, <2.5, and 33 nM, respectively, compared with those in μI channels of 1.4, 7.2, and 0.5 nM, respectively."
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"Thus, Lqh III is much more potent to remove fast inactivation of hH1 channels than Lqh II and LqhαIT."
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"Although under control conditions hH1 channels inactivate rapidly and completely, Lqh II and Lqh III at that low concentration strongly slowed down fast inactivation of hH1 channels."
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"We also studied the rates of fast inactivation of SkM1 and SCN5A. We took the falling phase (starting from around 2/3 of the maximal current to full inactivation, xref ) of Na + current measured in the activation experiment, and then fit the data with an exponential function to get a time constant (τ) of inactivation at each membrane potential ( xref )."
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"In the chimaeras, activation resembled that of mu1, fast inactivation resembled that of hH1, and steady-state fast inactivation fell between that of hH1 and mu1."
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"Thus, Lqh III not only removes fast inactivation of hH1 channels at lower concentrations, but also slows down inactivation more extensively than the other two toxins tested."
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"Lqh Toxins Modify Activation and Fast Inactivation of hH1 Channels."
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"In the control, fast inactivation of hH1 channels after 5 ms increases with increasing test voltage, and is complete at ∼0 mV."
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"After obtaining stable toxin effects at a concentration of 100 nM, toxin dissociation rates in hH1 channels were obtained in a voltage range from +20 to +180 mV with protocols like that shown in xref A. As shown in xref (B and C) a 100-ms dissociation pulse to +120 mV almost completely removed the effects of 100 nM Lqh II and LqhαIT on fast inactivation of hH1 channels, whereas a 540-ms dissociation pulse to the same voltage only partially removed the effects of Lqh III on fast inactivation."
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