Cryo-EM reveals an unprecedented binding site for Na(V)1.7 inhibitors enabling rational design of potent hybrid inhibitors

The voltage-gated sodium (Na(V)) channel Na(V)1.7 has been identified as a potential novel analgesic target due to its involvement in human pain syndromes. However, clinically available Na(V) channel-blocking drugs are not selective among the nine Na(V) channel subtypes, Na(V)1.1–Na(V)1.9. Moreover,...

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Detalles Bibliográficos
Autores principales: Kschonsak, Marc, Jao, Christine C, Arthur, Christopher P, Rohou, Alexis L, Bergeron, Philippe, Ortwine, Daniel F, McKerrall, Steven J, Hackos, David H, Deng, Lunbin, Chen, Jun, Li, Tianbo, Dragovich, Peter S, Volgraf, Matthew, Wright, Matthew R, Payandeh, Jian, Ciferri, Claudio, Tellis, John C
Formato: Online Artículo Texto
Lenguaje:English
Publicado: eLife Sciences Publications, Ltd 2023
Materias:
Structural Biology and Molecular Biophysics
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10112885/
https://www.ncbi.nlm.nih.gov/pubmed/36975198
http://dx.doi.org/10.7554/eLife.84151

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10112885/
https://www.ncbi.nlm.nih.gov/pubmed/36975198
http://dx.doi.org/10.7554/eLife.84151

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