ArticleScientific reports2017
Insensitivity to pain induced by a potent selective closed-state Nav1.7 inhibitor.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 60 papers.
What it found
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Who cites it
60 citing papers in PubMed, 122 citations in OpenAlex.
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- The α/β3 complex of human voltage-gated sodium channel hNaJournal of molecular modeling · 2025Article
- Discordance between preclinical and clinical testing of Na V 1.7-selective inhibitors for pain.Pain · 2025Review
- The venom ofFrontiers in pharmacology · 2025Article
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- The road to evolution of ProTx2: how to be a subtype-specific inhibition of human NaFrontiers in pharmacology · 2024Article
- A novel approach to completely alleviate peripheral neuropathic pain in human patients: insights from preclinical data.Frontiers in neuroanatomy · 2024Review
- Venom-derived peptides for breaking through the glass ceiling of drug development.Frontiers in chemistry · 2024Review
- Lessons learned in translating pain knowledge into practice.Pain reports · 2023Article
- The Effect of Evogliptin Tartrate on Controlling Inflammatory Pain.Biomedicines · 2023Article
- Structure-function and rational design of a spider toxin Ssp1a at human voltage-gated sodium channel subtypes.Frontiers in pharmacology · 2023Article
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- Computational design of peptides to target NaeLife · 2022Article
- Biologically Active Peptides from Venoms: Applications in Antibiotic Resistance, Cancer, and Beyond.International journal of molecular sciences · 2022Review
- Inhibition of NaRSC medicinal chemistry · 2022Review
- A Drug Discovery Approach for an Effective Pain Therapy through Selective Inhibition of Nav1.7.International journal of molecular sciences · 2022Article
- Towards Structure-Guided Development of Pain Therapeutics Targeting Voltage-Gated Sodium Channels.Frontiers in pharmacology · 2022Review
- Druggability of Voltage-Gated Sodium Channels-Exploring Old and New Drug Receptor Sites.Frontiers in pharmacology · 2022Review
- Highly Parallelized, Multicolor Optogenetic Recordings of Cellular Activity for Therapeutic Discovery Applications in Ion Channels and Disease-Associated Excitable Cells.Frontiers in molecular neuroscience · 2022Article
Corrections and comments
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Authors and funding
18 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pain places a devastating burden on patients and society and current pain therapeutics exhibit limitations in efficacy, unwanted side effects and the potential for drug abuse and diversion. Although genetic evidence has clearly demonstrated that the voltage-gated sodium channel, Nav1.7, is critical to pain sensation in mammals, pharmacological inhibitors of Nav1.7 have not yet fully recapitulated the dramatic analgesia observed in Nav1.7-null subjects. Using the tarantula venom-peptide ProTX-II as a scaffold, we engineered a library of over 1500 venom-derived peptides and identified JNJ63955918 as a potent, highly selective, closed-state Nav1.7 blocking peptide. Here we show that JNJ63955918 induces a pharmacological insensitivity to pain that closely recapitulates key features of the Nav1.7-null phenotype seen in mice and humans. Our findings demonstrate that a high degree of selectivity, coupled with a closed-state dependent mechanism of action is required for strong efficacy and indicate that peptides such as JNJ63955918 and other suitably optimized Nav1.7 inhibitors may represent viable non-opioid alternatives for the pharmacological treatment of severe pain.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.