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CryoEM reveals unprecedented binding site for Na <sub>V</sub> 1.7 inhibitors enabling rational design of potent hybrid inhibitors

2022-11-10

Abstract excerpt

The voltage-gated sodium (NaV) channel NaV1.7 has been identified as a potential novel pain target due to its striking human genetics. However, clinically available drugs (e.g. lidocaine, carbamazepine, etc.) are not selective among the nine NaV channel subtypes, NaV1.1-NaV1.9, and the two currently known classes of NaV1.7 subtype-selective inhibitors (aryl- and acylsulfonamides) have undesirable characteristics t...

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Literature Corpus work
489512a4-de9a-553b-8628-efa53dc701a3
DOI
10.1101/2022.11.10.515983
Open publication

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CryoEM reveals unprecedented binding site for Na <sub>V</sub> 1.7 inhibitors enabling rational design of potent hybrid inhibitorsDOI 10.1101/2022.11.10.515983
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