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Further contracted intracellular gate in the presence of the site BIG-binding drugs. Left : Structural comparison of Na v 1.7-BPV and Na v 1.7-apo (silver). Middle : The pore radii of Na v 1.7 bound to different ligands are calculated in HOLE and tabulated. Right : The α→ π transition of S6 IV and rearrangement of the gating residues, such as Leu398, Leu964, Ile1457 and Ile1756 (shown as ball and sticks), in the presence of BPV lead to gate contraction. LCM and CBZ-bound structures display nearly identical conformations to that of Na v 1.7-BPV.
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