The Batrachotoxin Receptor on the Voltage-Gated Sodium Channel is Guarded by the Channel Activation Gate

2002 ◽  
Vol 61 (4) ◽  
pp. 905-912 ◽  
Author(s):  
Hong-Ling Li ◽  
David Hadid ◽  
David S. Ragsdale
Keyword(s):  
Sodium Channel ◽  
Channel Activation ◽  
Voltage Gated Sodium Channel ◽  
Voltage Gated ◽  
Activation Gate

scholarly journals Local Postsynaptic Voltage-Gated Sodium Channel Activation in Dendritic Spines of Olfactory Bulb Granule Cells

Neuron ◽  
2016 ◽  
Vol 89 (6) ◽  
pp. 1355
Author(s):  
Wolfgang G. Bywalez ◽  
Dinu Patirniche ◽  
Vanessa Rupprecht ◽  
Martin Stemmler ◽  
Andreas V.M. Herz ◽  
...  
Keyword(s):  
Olfactory Bulb ◽  
Sodium Channel ◽  
Dendritic Spines ◽  
Granule Cells ◽  
Channel Activation ◽  
Voltage Gated Sodium Channel ◽  
Voltage Gated ◽  
Sodium Channel Activation

scholarly journals Structures of closed and open states of a voltage-gated sodium channel

2017 ◽  
Vol 114 (15) ◽  
pp. E3051-E3060 ◽  
Author(s):  
Michael J. Lenaeus ◽  
Tamer M. Gamal El-Din ◽  
Christopher Ing ◽  
Karthik Ramanadane ◽  
Régis Pomès ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Full Range ◽  
Structural Basis ◽  
Ion Permeation ◽  
Voltage Gated Sodium Channel ◽  
Voltage Gated ◽  
Voltage Gated Sodium Channels ◽  
Gating Mechanism ◽  
Activation Gate ◽  
Open States

Bacterial voltage-gated sodium channels (BacNavs) serve as models of their vertebrate counterparts. BacNavs contain conserved voltage-sensing and pore-forming domains, but they are homotetramers of four identical subunits, rather than pseudotetramers of four homologous domains. Here, we present structures of two NaVAb mutants that capture tightly closed and open states at a resolution of 2.8–3.2 Å. Introduction of two humanizing mutations in the S6 segment (NaVAb/FY: T206F and V213Y) generates a persistently closed form of the activation gate in which the intracellular ends of the four S6 segments are drawn tightly together to block ion permeation completely. This construct also revealed the complete structure of the four-helix bundle that forms the C-terminal domain. In contrast, truncation of the C-terminal 40 residues in NavAb/1–226 captures the activation gate in an open conformation, revealing the open state of a BacNav with intact voltage sensors. Comparing these structures illustrates the full range of motion of the activation gate, from closed with its orifice fully occluded to open with an orifice of ∼10 Å. Molecular dynamics and free-energy simulations confirm designation of NaVAb/1–226 as an open state that allows permeation of hydrated Na+, and these results also support a hydrophobic gating mechanism for control of ion permeation. These two structures allow completion of a closed–open–inactivated conformational cycle in a single voltage-gated sodium channel and give insight into the structural basis for state-dependent binding of sodium channel-blocking drugs.

scholarly journals The Selectivity Filter of the Voltage-gated Sodium Channel Is Involved in Channel Activation

2001 ◽  
Vol 276 (30) ◽  
pp. 27831-27839 ◽  
Author(s):  
Karlheinz Hilber ◽  
Walter Sandtner ◽  
Oliver Kudlacek ◽  
Ian W. Glaaser ◽  
Eva Weisz ◽  
...  
Keyword(s):  
Sodium Channel ◽  
Selectivity Filter ◽  
Channel Activation ◽  
Voltage Gated Sodium Channel ◽  
Voltage Gated

scholarly journals Thrombin Facilitation of Voltage-Gated Sodium Channel Activation in Human Cardiomyocytes

Circulation ◽  
2002 ◽  
Vol 106 (16) ◽  
pp. 2098-2103 ◽  
Author(s):  
Caroline Pinet ◽  
Bruno Le Grand ◽  
Gareth W. John ◽  
Alain Coulombe
Keyword(s):  
Sodium Channel ◽  
Channel Activation ◽  
Voltage Gated Sodium Channel ◽  
Human Cardiomyocytes ◽  
Voltage Gated ◽  
Sodium Channel Activation

scholarly journals Local Postsynaptic Voltage-Gated Sodium Channel Activation in Dendritic Spines of Olfactory Bulb Granule Cells

Neuron ◽  
2015 ◽  
Vol 85 (3) ◽  
pp. 590-601 ◽  
Author(s):  
Wolfgang G. Bywalez ◽  
Dinu Patirniche ◽  
Vanessa Rupprecht ◽  
Martin Stemmler ◽  
Andreas V.M. Herz ◽  
...  
Keyword(s):  
Olfactory Bulb ◽  
Sodium Channel ◽  
Dendritic Spines ◽  
Granule Cells ◽  
Channel Activation ◽  
Voltage Gated Sodium Channel ◽  
Voltage Gated ◽  
Sodium Channel Activation

The Voltage-Gated Sodium Channel Nav1.2 Contributes to Neurodegeneration in an Animal Model of Multiple Sclerosis

2016 ◽  
Vol 47 (S 01) ◽  
Author(s):  
W. Fazeli ◽  
B. Schattling ◽  
B. Engeland ◽  
M. Friese ◽  
D. Isbrand
Keyword(s):  
Multiple Sclerosis ◽  
Animal Model ◽  
Sodium Channel ◽  
Voltage Gated Sodium Channel ◽  
Voltage Gated
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