IndraLab

Statements

Gate activates KCNH2. 8 / 8
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"This suggests that the structure of the hERG activation gate and its coupling to the voltage sensing unit is different from that in Kv channels such as Shaker."
22586397
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"Subsequent studies showed that cross linking of cysteine residues engineered at D540 in the S4-S5 linker and L666 in the distal S6 segment stabilized the closed conformation of the hERG activation gate."
22586397
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"This would place the gate more than one helical turn below that described in Kir3.4 (24) and Shaker (11,12) channels and is consistent with previous predictions of hERG activation gate architecture (1[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
24606930
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"Most likely, the activation gate in the HERG channel is similar to the activation gate in the Kv channels, because the HERG activation gate can trap intracellular blockers in a similar manner to the activation gate in Kv channels."
12356850
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"Based upon the observation that the dependence of binding on the presence of S6 aromatic residues was decreased when inactivation was reduced by the S631A mutation 20, a model was proposed in which high affinity drug coordination requires conformational rearrangements associated with inactivation in addition to opening of the hERG activation gate 20."
29563525
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"This is of principal interest, because hERG channels are targeted by many pharmaceutical agents, the majority of which block by entering the pore via the intracellular activation gate and are limited [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
24606930
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"Here, we define the location of the hERG activation gate by introducing a proline induced kink at positions along the length of the inner S6 helix from, Ile 655 to Tyr 667."
24606930
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"This ligand and receptor model implies that when S4-S5 L is absent, the hERG activation gate should be in the open state, independent of the potential, as observed in one potassium 22 and one sodium 23 bacterial channels."
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