The pharmacology of voltage-gated sodium channel activators

JR Deuis, A Mueller, MR Israel, I Vetter - Neuropharmacology, 2017 - Elsevier
Toxins and venom components that target voltage-gated sodium (Na V) channels have
evolved numerous times due to the importance of this class of ion channels in the normal …

[HTML][HTML] Structural basis of Nav1. 7 inhibition by a gating-modifier spider toxin

H Xu, T Li, A Rohou, CP Arthur, F Tzakoniati, E Wong… - Cell, 2019 - cell.com
Voltage-gated sodium (Nav) channels are targets of disease mutations, toxins, and
therapeutic drugs. Despite recent advances, the structural basis of voltage sensing …

Targeted therapies for skeletal muscle ion channelopathies: systematic review and steps towards precision medicine

JF Desaphy, C Altamura, S Vicart… - Journal of …, 2021 - content.iospress.com
Background: Skeletal muscle ion channelopathies include non-dystrophic myotonias (NDM),
periodic paralyses (PP), congenital myasthenic syndrome, and recently identified congenital …

Aberrant epilepsy-associated mutant Nav1.6 sodium channel activity can be targeted with cannabidiol

RR Patel, C Barbosa, T Brustovetsky, N Brustovetsky… - Brain, 2016 - academic.oup.com
Mutations in brain isoforms of voltage-gated sodium channels have been identified in
patients with distinct epileptic phenotypes. Clinically, these patients often do not respond …

Structural basis for high-affinity trapping of the NaV1. 7 channel in its resting state by tarantula toxin

G Wisedchaisri, L Tonggu, TMG El-Din, E McCord… - Molecular cell, 2021 - cell.com
Voltage-gated sodium channels initiate electrical signals and are frequently targeted by
deadly gating-modifier neurotoxins, including tarantula toxins, which trap the voltage sensor …

Cardiac sodium channel palmitoylation regulates channel availability and myocyte excitability with implications for arrhythmia generation

Z Pei, Y Xiao, J Meng, A Hudmon… - Nature communications, 2016 - nature.com
Cardiac voltage-gated sodium channels (Nav1. 5) play an essential role in regulating
cardiac electric activity by initiating and propagating action potentials in the heart. Altered …

Voltage-gated Na+ channels: not just for conduction

LC Kruger, LL Isom - Cold Spring Harbor perspectives in …, 2016 - cshperspectives.cshlp.org
Voltage-gated sodium channels (VGSCs), composed of a pore-forming α subunit and up to
two associated β subunits, are critical for the initiation of the action potential (AP) in excitable …

A selective NaV1. 1 activator with potential for treatment of Dravet syndrome epilepsy

CY Chow, YKY Chin, L Ma, EAB Undheim… - Biochemical …, 2020 - Elsevier
Dravet syndrome (DS) is a catastrophic epileptic encephalopathy characterised by
childhood-onset polymorphic seizures, multiple neuropsychiatric comorbidities, and …

The sea anemone neurotoxins modulating sodium channels: an insight at structure and functional activity after four decades of investigation

MM Monastyrnaya, RS Kalina, EP Kozlovskaya - Toxins, 2022 - mdpi.com
Many human cardiovascular and neurological disorders (such as ischemia, epileptic
seizures, traumatic brain injury, neuropathic pain, etc.) are associated with the abnormal …

Spider toxin inhibits gating pore currents underlying periodic paralysis

R Männikkö, ZO Shenkarev, MG Thor… - Proceedings of the …, 2018 - National Acad Sciences
Gating pore currents through the voltage-sensing domains (VSDs) of the skeletal muscle
voltage-gated sodium channel NaV1. 4 underlie hypokalemic periodic paralysis (HypoPP) …