IndraLab

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Sodium atom inhibits KCNH2. 17 / 17
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"Most voltage gated K + currents are relatively insensitive to extracellular Na + (Na + o), but Na + o potently inhibits outward human ether-a-go-go-related gene (HERG)-encoded K + channel current (Numaguchi, H., J.P. Johnson, Jr., C.I. Petersen, and J.R. Balser."
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"We further found that the hERG Na + current can be blocked by external Na +, and the residues in the channel pore and S6 regions, including the serine residues at 624 and 641 as well as the phenylalanine in the signature motif of the selectivity filter, are involved in the block."
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"In addition to these direct anti-chaperone effects on HERG processing, the Na + / K + ATPase inhibitor digoxin indirectly disrupts HERG biogeneisis via a [K+] i -dependent conformational defect in HERG folding [XREF_BIBR], underscoring the intricacies of studying pharmacological chaperoning."
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"The data suggest that Ba 2+ sweeps Na + o from the pore as it exits inactivated HERG channels (XREF_FIG B, cartoon)."
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"Quantitatively similar effects of Na + i to inhibit HERG current were seen in the WT and S624A channels."
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"External Na + has been reported to block hERG K + current and the S624 residue was believed to be involved in the block."
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"Inhibition of the hERG Na + Current by External Na + Ions."
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"Although the physiological relevance of Na + i block in other K + channels has remained somewhat unclear, a functional role for block of HERG by Na + i can be rationalized in a satisfying way."
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"The Na + o block of hERG K + currents has been reported previously, and the IC 50 value for Na + o to block the hERG Na + current is close to that for Na + o to block hERG K + currents."
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"Since the F627Y and S641A significantly accelerated hERG inactivation, whereas S624A slightly decelerated it, inactivation gating seems not to be involved in the Na + o block of hERG channels."
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"XREF_BIBR Cardiac glycosides (XREF_FIG), specifically Na + / K + -ATPase inhibitors with known QT prolongation risk, reduce hERG trafficking in HEK293 lines and in guinea pig ventricular cardiomyocytes."
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"Physiologic [Na +] i blocks HERG current at depolarized potentials (XREF_FIG) and block is relieved by physiologic [K +] o (XREF_FIG)."
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"(d) C-type inactivation in Shaker is associated with a decrease in P K / P Na, whereas in HERG a disruption of C-type inactivation is associated with a decrease in P K / P Na (this report)."
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"We also found that external Na + potently blocked the hERG outward Na + current with an IC 50 of 3.5 mM."
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"Our experiments in this study support the conclusion that Na + o inhibits HERG current by binding to an outer pore site."
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"Na + Permeation through Inactivated hERG Channels."
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"Although Na + o blocked hERG Na + current, a robust outward hERG Na + current indicates that intracellular Na + (Na + i) does not block the channels."
16769794