Voltage-gated sodium channels (Na<sub>V</sub>) in GtoPdb v.2021.3

Abstract


Sodium channels are voltage-gated sodium-selective ion channels present in the membrane of most excitable cells. Sodium channels comprise of one pore-forming α subunit, which may be associated with either one or two β subunits [177]. α-Subunits consist of four homologous domains (I-IV), each containing six transmembrane segments (S1-S6) and a pore-forming loop. The positively charged fourth transmembrane segment (S4) acts as a voltage sensor and is involved in channel gating. The crystal structure of the bacterial NavAb channel has revealed a number of novel structural features compared to earlier potassium channel structures including a short selectivity filter with ion selectivity determined by interactions with glutamate side chains [274]. Interestingly, the pore region is penetrated by fatty acyl chains that extend into the central cavity which may allow the entry of small, hydrophobic pore-blocking drugs [274]. Auxiliary β1, β2, β3 and β4 subunits consist of a large extracellular N-terminal domain, a single transmembrane segment and a shorter cytoplasmic domain.

The nomenclature for sodium channels was proposed by Goldin et al., (2000) [144] and approved by the NC-IUPHAR Subcommittee on sodium channels (Catterall et al., 2005, [52]).

Published
02-Sep-2021
How to Cite
Catterall, W. A., Goldin, A. L. and Waxman, S. G. (2021) “Voltage-gated sodium channels (Na<sub>V</sub&gt;) in GtoPdb v.2021.3”, IUPHAR/BPS Guide to Pharmacology CITE, 2021(3). doi: 10.2218/gtopdb/F82/2021.3.
Section
Summaries