Towards Structure-Guided Development of Pain Therapeutics Targeting Voltage-Gated Sodium Channels
Voltage-gated sodium (NaV) channels are critical molecular determinants of action potential generation and propagation in excitable cells. Normal NaV channel function disruption can affect physiological neuronal signaling and lead to increased ...
Phuong T. Nguyen +2 more
doaj +1 more source
Genetics update: monogenetics, polygene disorders and the quest for modifying genes [PDF]
The genetic channelopathies are a broad collection of diseases. Many ion channel genes demonstrate wide phenotypic pleiotropy, but nonetheless concerted efforts have been made to characterise genotype-phenotype relationships.
Symonds, Joseph D., Zuberi, Sameer M.
core +1 more source
Nerve growth factor enhances voltage-gated Na+ channel activity and transwell migration in Mat-LyLu rat prostate cancer cell line [PDF]
The highly dynamic nature of voltage-gated Na+ channel (VGSC) expression and its controlling mechanism(s) are not well understood. In this study, we investigated the possible involvement of nerve growth factor (NGF) in regulating VGSC activity in the ...
Brackenbury, William J. +1 more
core +1 more source
p.L1612P, a Novel Voltage-gated Sodium Channel Nav1.7 Mutation Inducing a Cold Sensitive Paroxysmal Extreme Pain Disorder [PDF]
AbstractAbstract A new mutation, p.L1612P, was found in four family members suffering from Paroxysmal Extreme Pain Disorder. The mutant ion channel possesses unique electrophysiological characteristics, and a pharmacological profile distinct from other known mutations. Background: Mutations in the SCN9A gene
Suter, Marc +9 more
openaire +3 more sources
Pharmacogenetics of analgesic drugs [PDF]
• Individual variability in pain perception and differences in the efficacy of analgesic drugs are complex phenomena and are partly genetically predetermined.
Branford, R +4 more
core +1 more source
Human embryonic kidney (HEK293) cells express endogenous voltage-gated sodium currents and Nav1.7 sodium channels [PDF]
Human embryonic kidney (HEK293) cells are widely used for the heterologous expression of voltage- and ligand-gated ion channels. Patch clamp analysis of HEK293 cells in the whole-cell configuration identified voltage-gated, rapidly inactivating inward currents. Peak current amplitudes ranged from less than 100 pA to more than 800 pA, with the majority (
Bingjun, He, David M, Soderlund
openaire +2 more sources
Basic aspects of the pharmacodynamics of tolperisone, a widely applicable centrally acting muscle relaxant [PDF]
Tolperisone (2-methyl-1-(4-methylphenyl)-3-piperidin-1-ylpropan-1-one hydro-chloride) was introduced in the clinical practice more than forty years ago and is still evaluated as a widely applicable compound in pathologically elevated skeletal muscle tone
Bajaj P +36 more
core +1 more source
Parallel Evolution of Tetrodotoxin Resistance in Three Voltage-Gated Sodium Channel Genes in the Garter Snake Thamnophis sirtalis [PDF]
Members of a gene family expressed in a single species often experience common selection pressures. Consequently, the molecular basis of complex adaptations may be expected to involve parallel evolutionary changes in multiple paralogs.
Brodie, Edmund D. +6 more
core +1 more source
Objective: to analyze the interaction of cannabidiol (CBD) with Nav1.7 and compare it with carbamazepine (CBZ) through molecular docking. Methodology: a quantitative and experimental research, of the in silico type, which used CBD (CID: 644019) and CBZ (CID: 2554, standard drug blocker), anticonvulsant used in chronic pain, on the Nav1.7 channel (PDB ...
Gidelson José da Silva Júnior +6 more
openaire +1 more source
Compartment-specific regulation of NaV1.7 in sensory neurons after acute exposure to TNF-α
Summary: Tumor necrosis factor α (TNF-α) is a major pro-inflammatory cytokine, important in many diseases, that sensitizes nociceptors through its action on a variety of ion channels, including voltage-gated sodium (NaV) channels. We show here that TNF-α
Sidharth Tyagi +11 more
doaj +1 more source

