Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

Cryo-EM reveals an unprecedented binding site for NaV1.7 inhibitors enabling rational design of potent hybrid inhibitors

The voltage-gated sodium (NaV) channel NaV1.7 has been identified as a potential novel analgesic target due to its involvement in human pain syndromes. However, clinically available NaV channel-blocking drugs are not selective among the nine NaV channel subtypes, NaV1.1–NaV1.9. Moreover, the two cur...

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Bibliographic Details
Main Authors: Marc Kschonsak, Christine C Jao, Christopher P Arthur, Alexis L Rohou, Philippe Bergeron, Daniel F Ortwine, Steven J McKerrall, David H Hackos, Lunbin Deng, Jun Chen, Tianbo Li, Peter S Dragovich, Matthew Volgraf, Matthew R Wright, Jian Payandeh, Claudio Ciferri, John C Tellis
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2023-03-01
Series:eLife
Subjects:
Nav 1.7
sodium channel
pain
drug discovery
cryo-EM
Online Access:https://elifesciences.org/articles/84151

Internet

https://elifesciences.org/articles/84151

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