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

Non-SUMOylated CRMP2 decreases NaV1.7 currents via the endocytic proteins Numb, Nedd4-2 and Eps15

(2021) Kimberly Gomez et al.   Molecular Brain

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

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

Why are sodium channel modulators not yet pharmacotherapeutic trailblazers for neuropathic pain?

(2021) Anthony Dickenson   EXPERT OPINION ON PHARMACOTHERAPY

The physiological function of different voltage-gated sodium channels in pain

(2021) George Goodwin et al.   NATURE REVIEWS NEUROSCIENCE

A central mechanism of analgesia in mice and humans lacking the sodium channel NaV1.7

(2021) Donald Iain MacDonald et al.   NEURON

Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays

(2021) Richard L. Kraus et al.   Science Translational Medicine

Pharmacological characterization of a rat Nav1.7 loss-of-function model with insensitivity to pain

(2020) Lubin Chen et al.   PAIN

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

Anti-allodynic effects of the selective NaV1.7 inhibitor Pn3a in a mouse model of acute post-surgical pain

(2019) Alexander Mueller et al.   PAIN

The role of Nav1.7 in human nociceptors

(2019) Jannis E. Meents et al.   PAIN

Defining the Functional Role of NaV1.7 in Human Nociception

(2019) Lucy A. McDermott et al.   NEURON

Reversal of Peripheral Neuropathic Pain by the Small-Molecule Natural Product Physalin F via Block of CaV2.3 (R-Type) and CaV2.2 (N-Type) Voltage-Gated Calcium Channels

(2019) Zhiming Shan et al.   ACS Chemical Neuroscience

A small molecule targeting TDP-43’s RNA recognition motifs reduces locomotor defects in a Drosophila model of ALS

(2019) Liberty Francois-Moutal et al.   ACS Chemical Biology

Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study in Healthy Volunteers

(2019) Michael E. Rothenberg et al.   CLINICAL DRUG INVESTIGATION

[EXPRESS] Rat NaV1.7 loss-of-function genetic model: deficient nociceptive and neuropathic pain behavior with retained olfactory function and intra-epidermal nerve fibers

(2019) Barbara Grubinska et al.   Molecular Pain

The Natural Flavonoid Naringenin Elicits Analgesia through Inhibition of NaV1.8 Voltage-Gated Sodium Channels

(2019) Yuan Zhou et al.   ACS Chemical Neuroscience

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

The Blood–Brain Barrier (BBB) Score

(2019) Mayuri Gupta et al.   JOURNAL OF MEDICINAL CHEMISTRY

PKA-RII subunit phosphorylation precedes activation by cAMP and regulates activity termination

(2018) Jörg Isensee et al.   JOURNAL OF CELL BIOLOGY

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

GpTx-1 and [Ala5 , Phe6 , Leu26 , Arg28 ]GpTx-1, two peptide NaV 1.7 inhibitors: analgesic and tolerance properties at the spinal level

(2018) Chao Chen et al.   BRITISH JOURNAL OF PHARMACOLOGY

Chemical shift perturbation mapping of the Ubc9-CRMP2 interface identifies a pocket in CRMP2 amenable for allosteric modulation of Nav1.7 channels

(2018) Liberty François-Moutal et al.   Channels

(−)-Hardwickiic Acid and Hautriwaic Acid Induce Antinociception via Blockade of Tetrodotoxin-Sensitive Voltage-Dependent Sodium Channels

(2018) Song Cai et al.   ACS Chemical Neuroscience

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

Comparison of ex vivo and in vitro actions of gabapentin in superficial dorsal horn and the role of extra-spinal sites of drug action

(2018) Sascha R.A. Alles et al.   NEUROSCIENCE LETTERS

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

Acute anti-allodynic action of gabapentin in dorsal horn and primary somatosensory cortex: Correlation of behavioural and physiological data

(2017) Sascha R.A. Alles et al.   NEUROPHARMACOLOGY

Peripheral neuropathic pain

(2017) Ralf Baron et al.   PAIN

Long-lasting antinociceptive effects of green light in acute and chronic pain in rats

(2017) Mohab M. Ibrahim et al.   PAIN

Synergistic regulation of serotonin and opioid signaling contributes to pain insensitivity in Nav1.7 knockout mice

(2017) Jörg Isensee et al.   Science Signaling

Synergistic regulation of serotonin and opioid signaling contributes to pain insensitivity in Nav1.7 knockout mice

(2017) Jörg Isensee et al.   Science Signaling

Nav1.7 and other voltage-gated sodium channels as drug targets for pain relief

(2016) Edward C Emery et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

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

Analgesic Effects of GpTx-1, PF-04856264 and CNV1014802 in a Mouse Model of NaV1.7-Mediated Pain

(2016) Jennifer Deuis et al.   Toxins

Novel SCN9A Mutations Underlying Extreme Pain Phenotypes: Unexpected Electrophysiological and Clinical Phenotype Correlations

(2015) E. C. Emery et al.   JOURNAL OF NEUROSCIENCE

Pharmacotherapy for neuropathic pain in adults: a systematic review and meta-analysis

(2015) Nanna B Finnerup et al.   LANCET NEUROLOGY

(S)-Lacosamide Binding to Collapsin Response Mediator Protein 2 (CRMP2) Regulates CaV2.2 Activity by Subverting Its Phosphorylation by Cdk5

(2015) Aubin Moutal et al.   MOLECULAR NEUROBIOLOGY

De novo expression of Nav1.7 in injured putative proprioceptive afferents: Multiple tetrodotoxin-sensitive sodium channels are retained in the rat dorsal root after spinal nerve ligation

(2015) T. Fukuoka et al.   NEUROSCIENCE

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

An Isoform-Specific Myristylation Switch Targets Type II PKA Holoenzymes to Membranes

(2015) Ping Zhang et al.   STRUCTURE

Endogenous opioids contribute to insensitivity to pain in humans and mice lacking sodium channel Nav1.7

(2015) Michael S. Minett et al.   Nature Communications

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

Regulating excitability of peripheral afferents: emerging ion channel targets

(2014) Stephen G Waxman et al.   NATURE NEUROSCIENCE

Sumoylation of p35 Modulates p35/Cyclin-Dependent Kinase (Cdk) 5 Complex Activity

(2014) Anja Büchner et al.   NEUROMOLECULAR MEDICINE

Human sensory neurons: Membrane properties and sensitization by inflammatory mediators

(2014) Steve Davidson et al.   PAIN

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

(2014) Jacinthe Gingras et al.   PLoS One

Regulation of synaptic plasticity and cognition by SUMO in normal physiology and Alzheimer's disease

(2014) Linda Lee et al.   Scientific Reports

Spectomycin B1 as a Novel SUMOylation Inhibitor That Directly Binds to SUMO E2

(2013) Mikako Hirohama et al.   ACS Chemical Biology

Histamine Modulation of Acute Nociception Involves Regulation of Nav1.8 in Primary Afferent Neurons in Mice

(2013) Jie Yu et al.   CNS Neuroscience & Therapeutics

Expression of sodium channel α subunits 1.1, 1.2 and 1.6 in rat hippocampus after kainic acid-induced epilepsy

(2013) Xin Qiao et al.   EPILEPSY RESEARCH

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

β1- and β3- voltage-gated sodium channel subunits modulate cell surface expression and glycosylation of Nav1.7 in HEK293 cells

(2013) Cédric J. Laedermann et al.   Frontiers in Cellular Neuroscience

The NaV1.7 sodium channel: from molecule to man

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

Structure and Allostery of the PKA RII  Tetrameric Holoenzyme

(2012) P. Zhang et al.   SCIENCE

Distinct Nav1.7-dependent pain sensations require different sets of sensory and sympathetic neurons

(2012) Michael S. Minett et al.   Nature Communications

Naloxone-precipitated morphine withdrawal behavior and brain IL-1β expression: Comparison of different mouse strains

(2011) Liang Liu et al.   BRAIN BEHAVIOR AND IMMUNITY

Loss-of-function mutations in sodium channel Nav1.7 cause anosmia

(2011) Jan Weiss et al.   NATURE

Development and Characterization of Novel Derivatives of the Antiepileptic Drug Lacosamide That Exhibit Far Greater Enhancement in Slow Inactivation of Voltage-Gated Sodium Channels

(2010) Yuying Wang et al.   ACS Chemical Neuroscience

Time course and specificity of the pharmacological disruption of the trafficking of voltage-gated calcium channels by gabapentin

(2010) Fay Heblich et al.   Channels

Single-cell analysis of sodium channel expression in dorsal root ganglion neurons

(2010) Cojen Ho et al.   MOLECULAR AND CELLULAR NEUROSCIENCE

Ginkgolic Acid Inhibits Protein SUMOylation by Blocking Formation of the E1-SUMO Intermediate

(2009) Isao Fukuda et al.   CHEMISTRY & BIOLOGY

Kerriamycin B inhibits protein SUMOylation

(2009) Isao Fukuda et al.   JOURNAL OF ANTIBIOTICS

ProTx-II, a Selective Inhibitor of NaV1.7 Sodium Channels, Blocks Action Potential Propagation in Nociceptors

(2008) W. A. Schmalhofer et al.   MOLECULAR PHARMACOLOGY

Pharmacological disruption of calcium channel trafficking by the  2  ligand gabapentin

(2008) J. Hendrich et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA