The DOI matches its Crossref record; 45 of the 46 references it cites were found in a registry or an index.
Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels
Open accessAbstract
Significance: Voltage-gated sodium (Na v ) channels contribute to physiological and pathophysiological electrical signaling in nerve and muscle cells. Because Na v channel isoforms exhibit tissue-specific expression, subtype selective modulation of this channel family provides important drug development opportunities. However, most available Na v channel modulators are unable to distinguish between Na v channel subtypes, which limits their therapeutic utility because of cardiac or nervous system toxicity. This study describes a new class of subtype selective Na v channel inhibitors that interact with a region of the channel that controls voltage sensitivity. This interaction site may enable development of selective therapeutic interventions with reduced potential for toxicity.
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“Since there is precedent for small molecule compounds that either enhance or diminish ion channel activity [60–62], it is conceivable to develop drugs for modulating NaV1.2 activity to treat IEE and ASD/ID.”
From Progress in Understanding and Treating SCN2A-Mediated Disorders (2018) · cites this paper as [60]
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Cites
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An SCN9A channelopathy causes congenital inability to experience pain
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The crystal structure of a voltage-gated sodium channel
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Molecular Determinants of State-Dependent Block of Na + Channels by Local Anesthetics
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Voltage‐gated sodium channels at 60: structure, function and pathophysiology
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Voltage-gated ion channels and gating modifier toxins
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Ion Channel Voltage Sensors: Structure, Function, and Pathophysiology
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The Role of Voltage-Gated Sodium Channels in Pain Signaling
Bennett, D. L., Clark, A. J., Huang, J., Waxman, S. G., & Dib-Hajj, S. D. (2019) · Physiological Reviews · doi:10.1152/physrev.00052.2017 · Cited by 730
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Progress in Understanding and Treating SCN2A-Mediated Disorders
Sanders, S. J., Campbell, A. J., Cottrell, J. R., Moller, R. S., Wagner, F. F., Auldridge, A. L., Bernier, R. A., Catterall, W. A., Chung, W. K., Empfield, J. R., et al. (2018) · Trends in Neurosciences · doi:10.1016/j.tins.2018.03.011 · Cited by 338
Metadata
- Authors
- McCormack, K., Santos, S., Chapman, M. L., Krafte, D. S., Marron, B. E., West, C. W., Krambis, M. J., Antonio, B. M., Zellmer, S. G., Printzenhoff, D., Padilla, K. M., Lin, Z., Wagoner, P. K., Swain, N. A., Stupple, P. A., de Groot, M., Butt, R. P., & Castle, N. A.
- Affiliations
- Pfizer (United States) (US)
- Pfizer (United Kingdom) (GB)
- Pfizer Ltd., Sandwich, Kent CT13 9NJ, United Kingdom
- ORCID
- Venue
- Proceedings of the National Academy of Sciences
- Publisher
- National Academy of Sciences
- Published
- 2013-07
- Volume
- 110
- Issue
- 29
- Pages
- E2724-32
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- PMC
- PMC3718154
- OpenAlex
- W1979671751
- Cited by
- 244
- References
- 46
- Citations by year
- 2026: 15 · 2025: 12 · 2024: 20 · 2023: 16 · 2022: 20 · 2021: 19 · 2020: 19 · 2019: 14 · 2018: 24 · 2017: 33 · 2016: 22 · 2015: 13 · 2014: 15 · 2013: 2
- FWCI
- 8.36
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Proceedings of the National Academy of Sciences (publishedVersion)
- Europe PMC (PubMed Central) (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Ion channel regulation and function
- Health Sciences › Medicine › Cardiology and Cardiovascular Medicine › Cardiac electrophysiology and arrhythmias
- Life Sciences › Neuroscience › Sensory Systems › Ion Channels and Receptors
- Keywords
- voltage-gated sodium channels, small molecule inhibitors, subtype selectivity, Nav1.3, Nav1.7, cardiac sodium channel, toxin binding site, alpha-scorpion toxin, species sensitivity, sodium channel inactivation
- MeSH terms
- Acetamides, Binding Sites, Humans, Molecular Sequence Data, Thiazoles, Sequence Alignment, Patch-Clamp Techniques, Inhibitory Concentration 50, Amino Acid Motifs, Electrophysiological Phenomena, HEK293 Cells, Voltage-Gated Sodium Channel Blockers, NAV1.3 Voltage-Gated Sodium Channel
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