Identification and targeting of a unique Na V 1.7 domain driving chronic pain

Small molecule targeting NaV1.7 via inhibition of the CRMP2-Ubc9 interaction reduces pain in chronic constriction injury (CCI) rats

(2022) Jiahe Li et al.   Channels

Long-lasting analgesia via targeted in situ repression of NaV1.7 in mice

(2021) Ana M. Moreno et al.   Science Translational Medicine

Selective targeting of NaV1.7 via inhibition of the CRMP2-Ubc9 interaction reduces pain in rodents

(2021) Song Cai et al.   Science Translational Medicine

Sensory neuron–derived NaV1.7 contributes to dorsal horn neuron excitability

(2020) Sascha R. A. Alles et al.   Science Advances

Studies on CRMP2 SUMOylation-deficient transgenic mice identify sex-specific NaV1.7 regulation in the pathogenesis of chronic neuropathic pain

(2020) Aubin Moutal et al.   PAIN

Design of Phase 3 Studies Evaluating Vixotrigine for Treatment of Trigeminal Neuralgia

(2020) Mona Kotecha et al.   Journal of Pain Research

SARS-CoV-2 Spike protein co-opts VEGF-A/Neuropilin-1 receptor signaling to induce analgesia

(2020) Aubin Moutal et al.   PAIN

AAV-encoded CaV2.2 peptide aptamer CBD3A6K for primary sensory neuron-targeted treatment of established neuropathic pain

(2019) Hongwei Yu et al.   GENE THERAPY

The Role of Voltage-Gated Sodium Channels in Pain Signaling

(2019) David L. Bennett et al.   PHYSIOLOGICAL REVIEWS

Lack of Detection of the Analgesic Properties of PF‐05089771, a Selective Na v 1.7 Inhibitor, Using a Battery of Pain Models in Healthy Subjects

(2019) Pieter Siebenga et al.   CTS-Clinical and Translational Science

Building sensory axons: Delivery and distribution of NaV1.7 channels and effects of inflammatory mediators

(2019) Elizabeth J. Akin et al.   Science Advances

Nav1.7 is phosphorylated by Fyn tyrosine kinase which modulates channel expression and gating in a cell type-dependent manner

(2018) Yangyang Li et al.   Molecular Pain

Efficacy of the Nav1.7 blocker PF-05089771 in a randomised, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy

(2018) Aoibhinn McDonnell et al.   PAIN

Inhibition of the Ubc9 E2 SUMO-conjugating enzyme–CRMP2 interaction decreases NaV1.7 currents and reverses experimental neuropathic pain

(2018) Liberty François-Moutal et al.   PAIN

Insensitivity to Pain upon Adult-Onset Deletion of Nav1.7 or Its Blockade with Selective Inhibitors

(2018) Shannon D. Shields et al.   JOURNAL OF NEUROSCIENCE

Phosphorylated CRMP2 Regulates Spinal Nociceptive Neurotransmission

(2018) Jie Yu et al.   MOLECULAR NEUROBIOLOGY

DRG Voltage-Gated Sodium Channel 1.7 Is Upregulated in Paclitaxel-Induced Neuropathy in Rats and in Humans with Neuropathic Pain

(2017) Yan Li et al.   JOURNAL OF NEUROSCIENCE

Safety and efficacy of a Nav1.7 selective sodium channel blocker in patients with trigeminal neuralgia: a double-blind, placebo-controlled, randomised withdrawal phase 2a trial

(2017) Joanna M Zakrzewska et al.   LANCET NEUROLOGY

Blocking CRMP2 SUMOylation reverses neuropathic pain

(2017) A Moutal et al.   MOLECULAR PSYCHIATRY

Na V 1.7 as a pain target – From gene to pharmacology

(2017) Irina Vetter et al.   PHARMACOLOGY & THERAPEUTICS

Voltage-gated Na+ currents in human dorsal root ganglion neurons

(2017) Xiulin Zhang et al.   eLife

Hierarchical CRMP2 posttranslational modifications control NaV1.7 function

(2016) Erik T. Dustrude et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

(2016) Aristos J. Alexandrou et al.   PLoS One

A membrane-delimited N-myristoylated CRMP2 peptide aptamer inhibits CaV2.2 trafficking and reverses inflammatory and postoperative pain behaviors

(2015) Liberty François-Moutal et al.   PAIN

Enhanced Excitability of Primary Sensory Neurons and Altered Gene Expression of Neuronal Ion Channels in Dorsal Root Ganglion in Paclitaxel-induced Peripheral Neuropathy

(2014) Haijun Zhang et al.   ANESTHESIOLOGY

Painful and painless channelopathies

(2014) David L H Bennett et al.   LANCET NEUROLOGY

Global Nav1.7 Knockout Mice Recapitulate the Phenotype of Human Congenital Indifference to Pain

(2014) Jacinthe Gingras et al.   PLoS One

Evaluation of behavior and expression of NaV1.7 in dorsal root ganglia after sciatic nerve compression and application of nucleus pulposus in rats

(2013) Michiaki Mukai et al.   EUROPEAN SPINE JOURNAL

CRMP2 Protein SUMOylation Modulates NaV1.7 Channel Trafficking

(2013) Erik T. Dustrude et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dysregulation of voltage-gated sodium channels by ubiquitin ligase NEDD4-2 in neuropathic pain

(2013) Cédric J. Laedermann et al.   JOURNAL OF CLINICAL INVESTIGATION

The NaV1.7 sodium channel: from molecule to man

(2012) Sulayman D. Dib-Hajj et al.   NATURE REVIEWS NEUROSCIENCE

The Pharmacokinetics of Cell-Penetrating Peptides

(2010) Dikran Sarko et al.   MOLECULAR PHARMACEUTICS