Hydropathicity-based prediction of pain-causing NaV1.7 variants [PDF]
Background Mutation-induced variations in the functional architecture of the NaV1.7 channel protein are causally related to a broad spectrum of human pain disorders. Predicting in silico the phenotype of NaV1.7 variant is of major clinical importance; it
Makros N. Xenakis +10 more
doaj +4 more sources
Pain without Nociceptors? Nav1.7-Independent Pain Mechanisms [PDF]
Nav1.7, a peripheral neuron voltage-gated sodium channel, is essential for pain and olfaction in mice and humans. We examined the role of Nav1.7 as well as Nav1.3, Nav1.8, and Nav1.9 in different mouse models of chronic pain.
Michael S. Minett +6 more
doaj +6 more sources
Structural mapping of Nav1.7 antagonists
Voltage-gated sodium (Nav) channels are targeted by a number of widely used and investigational drugs for the treatment of epilepsy, arrhythmia, pain, and other disorders.
Qiurong Wu +8 more
semanticscholar +4 more sources
Non-addictive treatment of chronic pain represents a major unmet clinical need. Peripheral voltage-gated sodium (NaV) channels are an attractive target for pain therapy because they initiate and propagate action potentials in primary afferents that ...
Sidharth Tyagi +22 more
doaj +2 more sources
Sensory neuron–expressed FGF13 controls nociceptive signaling in diabetic neuropathy models [PDF]
Nociception involves complex signaling, yet intrinsic mechanisms bidirectionally regulating this process remain unexplored. Here, we show that the fibroblast growth factor 13 (FGF13)/Nav1.7 protein–protein interaction (PPI) complex bidirectionally ...
Aditya K. Singh +49 more
doaj +2 more sources
Carbenoid-involved reactions integrated with scaffold-based screening generates a Nav1.7 inhibitor
The discovery of selective Nav1.7 inhibitors is a promising approach for developing anti-nociceptive drugs. In this study, we present a novel oxindole-based readily accessible library (OREAL), which is characterized by readily accessibility, unique ...
Jirong Shu +6 more
doaj +2 more sources
The parabss1 Drosophila melanogaster as Model for Chronic Nociception: Insights Into Cannabidiol Analgesic Effects. [PDF]
ABSTRACT Background Chronic pain, which is often unrelated to ongoing injury, is poorly understood and difficult to treat. Genetic studies have identified voltage‐gated sodium (Nav) channels, particularly gain‐of‐function mutations such as L858F and R1150W in human NaV1.7, as involved in the development of chronic pain. Methods A chronic pain model was
Malta SM +7 more
europepmc +2 more sources
Human Dorsal Root Ganglia Neuronal Cell Line to Study Nociceptive Signaling: A New Pipeline for Pain Therapy. [PDF]
The nociceptive properties of differentiated human HD10.6 cells were characterized by multiple approaches (A). Peripheral sensitization was induced within HD10.6 cells in response to an inflammatory cocktail (B), modeling nociceptors in a chronic pain state.
Dochnal SA +11 more
europepmc +2 more sources
Cell specific regulation of NaV1.7 activity and trafficking in rat nodose ganglia neurons
The voltage-gated sodium NaV1.7 channel sets the threshold for electrogenesis. Mutations in the gene encoding human NaV1.7 (SCN9A) cause painful neuropathies or pain insensitivity. In dorsal root ganglion (DRG) neurons, activity and trafficking of NaV1.7
Santiago I. Loya-López +6 more
doaj +1 more source
Varicella-Zoster viruses associated with post-herpetic neuralgia induce sodium current density increases in the ND7-23 Nav-1.8 neuroblastoma cell line [PDF]
Post-herpetic neuralgia (PHN) is the most significant complication of herpes zoster caused by reactivation of latent Varicella-Zoster virus (VZV). We undertook a heterologous infection in vitro study to determine whether PHN-associated VZV isolates ...
A Vafai +44 more
core +8 more sources

