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PHARMACOLOGY & THERAPEUTICS, ISSN 0163-7258, 04/2017, Volume 172, pp. 73 - 100
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 10/2018, Volume 28, Issue 19, pp. 3141 - 3149
The voltage gated sodium channel Na(v)1.7 plays an essential role in the transmission of pain signals. Strong human genetic validation has motivated extensive... 
CHEMISTRY, MEDICINAL | EFFICACY | GATED SODIUM-CHANNELS | CHEMISTRY, ORGANIC | DISCOVERY | POTENT | Pain | PHARMACOKINETICS | AFFINITY | SCN9A | SELECTIVE INHIBITORS | ARYL SULFONAMIDES | Voltage gated sodium channel | EFFICIENT | Na(v)1.7 | REVEALS
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 02/2019, Volume 29, Issue 4, pp. 659 - 663
Screening of 100 acylsulfonamides from the Bristol-Myers Squibb compound collection identified the C3-cyclohexyl indole 6 as a potent Na(v)1.7 inhibitor.... 
Acyl sulfonamide | POTENT | CHEMISTRY, MEDICINAL | Pain | EFFICACY | Indole-based | SCN9A | ARYL SULFONAMIDES | SELECTIVE INHIBITORS | CHEMISTRY, ORGANIC | OF-FUNCTION MUTATIONS | Na(v)1.7 inhibitor
Journal Article
PAIN, ISSN 0304-3959, 03/2018, Volume 159, Issue 3, pp. 496 - 506
Journal Article
PAIN, ISSN 0304-3959, 03/2018, Volume 159, Issue 3, pp. 469 - 480
Diabetic peripheral neuropathy (DPN) is a common disabling complication of diabetes. Almost half of the patients with DPN develop neuropathic pain (NeuP) for... 
SYSTEM | DEFINITION | DISORDER MUTATIONS | Electrophysiology | VALIDATION | PHENOTYPE | OF-FUNCTION MUTATIONS | NEUROSCIENCES | CLINICAL NEUROLOGY | Neuropathic pain | INACTIVATION | ERYTHROMELALGIA | Diabetic peripheral neuropathy | SCN9A VARIANTS | DOUBLE-BLIND | Genetics | ANESTHESIOLOGY | Voltage-gated sodium channel Na(V)1.7
Journal Article
SCIENTIFIC REPORTS, ISSN 2045-2322, 01/2017, Volume 7
Human genetic studies have implicated the voltage-gated sodium channel Na(V)1.7 as a therapeutic target for the treatment of pain. A novel peptide,... 
SPINAL SENSORY NEURONS | PAIN | ALPHA-SUBUNIT | ROOT GANGLION NEURONS | CHEMICAL-SHIFTS | MULTIDISCIPLINARY SCIENCES | GATED SODIUM-CHANNELS | DRG NEURONS | CLOSED-STATE INACTIVATION | NA-V | SCN9A MUTATIONS
Journal Article
EXPERT OPINION ON THERAPEUTIC TARGETS, ISSN 1472-8222, 08/2016, Volume 20, Issue 8, pp. 975 - 983
Introduction: Chronic pain is a massive clinical problem. We discuss the potential of subtype selective sodium channel blockers that may provide analgesia with... 
COMMON VARIANTS | pain | ROOT GANGLION NEURONS | SCN9A MUTATIONS | sensory neurons | OF-FUNCTION MUTATIONS | CURRENTS | Na(v)1 | MICE LACKING | NEUROPATHIC PAIN | PR INTERVAL | SCN9A | PHARMACOLOGY & PHARMACY | INFLAMMATORY PAIN | QRS DURATION | opioids
Journal Article
NEURON, ISSN 0896-6273, 03/2019, Volume 101, Issue 5, pp. 905 - 905
Loss-of-function mutations in Na(v)1.7 cause congenital insensitivity to pain (CIP); this voltage-gated sodium channel is therefore a key target for analgesic... 
PERIPHERAL-NERVE | NEUROPATHIC PAIN | SODIUM-CHANNEL NA(V)1.7 | C-NOCICEPTORS | CLOSED-STATE INACTIVATION | MEMBRANE-PROPERTIES | SCN9A MUTATIONS | OF-FUNCTION MUTATIONS | SKIN | NEUROSCIENCES | SENSORY NEURONS
Journal Article
EMBO JOURNAL, ISSN 0261-4189, 02/2018, Volume 37, Issue 3, pp. 427 - 445
The voltage-gated sodium channel Na(V)1.7 plays a critical role in pain pathways. We generated an epitope-tagged NaV1.7 mouse that showed normal pain... 
pain | BIOCHEMISTRY & MOLECULAR BIOLOGY | TRAFFICKING | VOLTAGE-GATED SODIUM | SUBUNITS | SENSORY NEURONS | CELL BIOLOGY | NEUROPATHIC PAIN | sensory neuron | sodium channel | CALCIUM-CHANNELS | PURIFICATION MASS-SPECTROMETRY | protein-protein interactor | Na(V)1.7 | AP-MS | EXPRESSION | MACROMOLECULAR COMPLEXES
Journal Article
PLOS ONE, ISSN 1932-6203, 03/2017, Volume 12, Issue 3
Venom-derived peptides have attracted much attention as potential lead molecules for pharmaceutical development. A well-known example is Huwentoxin-IV... 
COMMON MOLECULAR DETERMINANTS | NEUROPATHIC PAIN | PROTEIN BACKBONE | SODIUM-CHANNEL ANTAGONIST | MORPHINE | SPIDER SELENOCOSMIA-HUWENA | NMR CHEMICAL-SHIFTS | MULTIDISCIPLINARY SCIENCES | TARGET NA(V)1.7 | TORSION ANGLES | RAT FORMALIN TEST
Journal Article
BIOCHEMICAL PHARMACOLOGY, ISSN 0006-2952, 05/2019, Volume 163, pp. 9 - 20
The peripherally expressed voltage-gated sodium Na(v)1.7 (gene SCN9A) channel boosts small stimuli to initiate firing of pain-signaling dorsal root ganglia... 
Non-opioids | NAV1.7 | ROOT GANGLION NEURONS | GATED SODIUM-CHANNELS | Protein-interactome | Novel therapeutics | Chronic pain | MU-OPIOID RECEPTOR | MICE LACKING | NEUROPATHIC PAIN | CRMP2 | CHRONIC CONSTRICTION INJURY | PHARMACOLOGY & PHARMACY | PHOSPHATIDYLETHANOLAMINE-BINDING PROTEIN | EXPRESSION | Na(v)1.7
Journal Article
BRITISH JOURNAL OF PHARMACOLOGY, ISSN 0007-1188, 05/2015, Volume 172, Issue 10, pp. 2445 - 2458
Background and PurposeChronic pain is a serious worldwide health issue, with current analgesics having limited efficacy and dose-limiting side effects. Humans... 
PHARMACOLOGY | EXTREME PAIN DISORDER | NA-V | PHARMACOLOGY & PHARMACY | MUTATIONS | VOLTAGE-SENSOR | SODIUM-CHANNEL | HUWENTOXIN-IV | NUCLEOTIDE POLYMORPHISM | BINDING | PEPTIDE TOXINS
Journal Article
CLINICAL GENETICS, ISSN 0009-9163, 04/2007, Volume 71, Issue 4, pp. 311 - 319
Congenital indifference to pain (CIP) is a rare condition in which patients have severely impaired pain perception, but are otherwise essentially normal. We... 
pain | ERYTHERMALGIA | SCLEROSTEOSIS | SENSORY NEURONS | INSENSITIVITY | mutation | SODIUM-CHANNEL BLOCKERS | genetics | sodium channel | CIP (congenital indifference to pain) | SCN9A | AUTONOMIC NEUROPATHIES | GENETICS & HEREDITY | DISORDER | HSAN | LINKAGE ANALYSIS | Na(v)1.7 | ANALGESIA
Journal Article
BRAIN, ISSN 0006-8950, 02/2019, Volume 142, pp. 263 - 275
Symptomatic treatment of neuropathic pain in small fibre neuropathy is often disappointing. The finding of voltage-gated sodium channel mutations in small... 
RCT | EFFICACY | SAFETY | SODIUM-CHANNELS | 7 mutations | Na(v)1 | NEUROSCIENCES | SLOW-INACTIVATION | CLINICAL NEUROLOGY | PATHOPHYSIOLOGY | neuropathic pain | PAIN | lacosamide | CRMP2 | small fibre neuropathy | DOUBLE-BLIND
Journal Article
JOURNAL OF MEDICINAL CHEMISTRY, ISSN 0022-2623, 03/2017, Volume 60, Issue 6, pp. 2513 - 2525
By taking advantage of certain features in piperidine 4, we developed a novel series of cyclohexylamine-and piperidine-based benzenesulfonamides as potent and... 
SODIUM-CHANNEL NA(V)1.7 | CHEMISTRY, MEDICINAL | SCN9A | OF-FUNCTION MUTATIONS | ANTAGONISTS | DISCOVERY
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 05/2017, Volume 27, Issue 10, pp. 2087 - 2093
The voltage-gated sodium channel Na(v)1.7 is a genetically validated target for the treatment of pain with gain-of-function mutations in man eliciting a... 
CHEMISTRY, MEDICINAL | CHEMISTRY, ORGANIC | Selectivity | Ion channel | Arylsulfonamide | P-GLYCOPROTEIN | NEUROPATHIC PAIN | Pain | CHANNEL | LIDOCAINE | SCN9A | DRUGS | VOLTAGE SENSOR | MUTATIONS | Na(v)1.7
Journal Article
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ISSN 0960-894X, 03/2018, Volume 28, Issue 5, pp. 958 - 962
Replacement of the piperidine ring in the lead benzenesulfonamide Na(v)1.7 inhibitor 1 with a weakly basic morpholine core resulted in a significant reduction... 
CHEMISTRY, MEDICINAL | EFFICACY | CHEMISTRY, ORGANIC | OF-FUNCTION MUTATIONS | Na(v)1.7 inhibitor | Morpholine-based | SODIUM-CHANNEL NA(V)1.7 | POTENT | Pain | MODELS | SCN9A | SELECTIVE INHIBITORS | Aryl sulfonamides
Journal Article
PAIN, ISSN 0304-3959, 10/2018, Volume 159, Issue 10, pp. 2115 - 2127
We previously reported that destruction of the small ubiquitin-like modifier (SUMO) modification site in the axonal collapsin response mediator protein 2... 
RESPONSE MEDIATOR PROTEIN-2 | PHOSPHORYLATION | SUMOylation motif decoy | GATED SODIUM-CHANNELS | POSTTRANSLATIONAL MODIFICATIONS | NERVE INJURY | NEUROSCIENCES | SUMOYLATION | CLINICAL NEUROLOGY | Neuropathic pain | CRMP2 | VOLTAGE SENSOR | PERIPHERAL NEUROPATHY | ANESTHESIOLOGY | Na(V)1.7 | MUTATIONS
Journal Article
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