The DOI matches its Crossref record; 2 of the 2 references it cites were found in a registry or an index.
Discovery of a selective Na V 1.7 inhibitor from centipede venom with analgesic efficacy exceeding morphine in rodent pain models
Open accessAbstract
Significance: The economic burden of chronic pain in the United States is currently ∼$600 billion per annum, which exceeds the combined annual cost of cancer, heart disease, and diabetes. Few drugs are available for treating chronic pain, and many have limited efficacy and dose-limiting side-effects. Humans with inheritable loss-of-function mutations in the voltage-gated sodium channel Na V 1.7 are indifferent to all types of pain, and therefore drugs that block this channel should be useful analgesics for treating many pain conditions. Herein we describe Ssm6a, a peptide from centipede venom that potently and selectively blocks the human Na V 1.7 channel. Ssm6a proved to be more analgesic than morphine in rodent pain models and did not cause any side-effects.
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Cites
Overview of the voltage-gated sodium channel family
Yu (2003) · Genome biology · doi:10.1186/gb-2003-4-3-207 · Cited by 694
Sodium channel Na v 1.6 is localized at nodes of Ranvier, dendrites, and synapses
Caldwell, J. H., Schaller, K. L., Lasher, R. S., Peles, E., & Levinson, S. R. (2000) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.090034797 · Cited by 649
Cited by
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
Voltage-gated sodium channels: structure, function, pharmacology, and clinical indications
de Lera Ruiz, M., & Kraus, R. L. (2015) · Journal of Medicinal Chemistry · doi:10.1021/jm501981g · Cited by 548
Neural circuits for pain: Recent advances and current views
Peirs, C., & Seal, R. P. (2016) · Science · doi:10.1126/science.aaf8933 · Cited by 478
Metadata
- Authors
- Yang, S., Xiao, Y., Kang, D., Liu, J., Li, Y., Undheim, E. A. B., Klint, J. K., Rong, M., Lai, R., & King, G. F.
- Venue
- Proceedings of the National Academy of Sciences
- Published
- 2013-09-30
- Volume
- 110
- Issue
- 43
- Pages
- 17534-17539
- ISSN
- 0027-8424 (ISSN-L)
- 1091-6490
- OpenAlex
- W2154594506
- Cited by
- 177
- References
- 2
- FWCI
- 12.16
- Type
- journal article
- Language
- en
- Open access
- green
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- Yang, S., Xiao, Y., Kang, D., Liu, J., Li, Y., Undheim, E. A. B., Klint, J. K., Rong, M., Lai, R., & King, G. F. (2013). Discovery of a selective Na V 1.7 inhibitor from centipede venom with analgesic efficacy exceeding morphine in rodent pain models. Proceedings of the National Academy of Sciences. https://doi.org/10.1073/pnas.1306285110
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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