IndraLab

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HaTx inhibits KCNB1. 6 / 6
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"To test further if the substituting KcsA pore is indeed under the control of the voltage sensors, we made a chimera between KcsA and the DRK1 (K V 2.1) voltage gated K + channel, because DRK1 is inhibited by HaTx."
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"Thus, HaTx inhibits the drk1 K+ channel, not by physically occluding the ion conduction pore, but by modifying channel gating."
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"For example, Hanatoxin (HaTx), a peptide isolated from tarantula venom, inhibits Kv2.1 (Swartz and MacKinnon, 1997) but activates Kv1.2 (Milescu et al., 2013)."
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"HaTx markedly inhibits Kv2.1 ionic current when it binds to only one of four channel subunits; full efficacy is achieved when HaTx binds to all four subunits, and each subunit appears to bind HaTx independently (Swartz and MacKinnon, 1997a; Lee et al., 2003; Phillips et al., 2005)."
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"Since HaTx inhibits DRK1 by hindering the movement of gating charges, the HaTx sensitivity of the chimera indicates that its gate remains under control of the voltage sensors."
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"We studied the mechanism by which Hanatoxin (HaTx) inhibits the drk1 voltage gated K+ channel."
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