Discovery of Selective Inhibitors of Na<sub>V</sub>1.7 Templated on Saxitoxin as Therapeutics for Pain-Reference-Cited by-同舟云学术

Discovery of Selective Inhibitors of Na_V1.7 Templated on Saxitoxin as Therapeutics for Pain

Published:2022-10-18 Issue:11 Volume:13 Page:1763-1768
ISSN:1948-5875
Container-title:ACS Medicinal Chemistry Letters
language:en
Short-container-title:ACS Med. Chem. Lett.

Author:

Pajouhesh Hassan¹,Delwig Anton¹,Beckley Jacob T.²,Klas Sheri²,Monteleone Dennis¹^ORCID,Zhou Xiang¹,Luu George¹,Du Bois J.³^ORCID,Hunter John C.¹^ORCID,Mulcahy John V.¹^ORCID

Affiliation:

1. SiteOne Therapeutics, Inc., South San Francisco, California 94080, United States

2. SiteOne Therapeutics, Inc., Bozeman, Montana 59715, United States

3. Department of Chemistry, Stanford University, Stanford, California 94305, United States

Funder

U.S. Department of Health and Human Services

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acsmedchemlett.2c00378

Reference17 articles.

1. An SCN9A channelopathy causes congenital inability to experience pain

2. Loss-of-function mutations in the Nav1.7 gene underlie congenital indifference to pain in multiple human populations

3. Slow Closed-State Inactivation: A Novel Mechanism Underlying Ramp Currents in Cells Expressing the hNE/PN1 Sodium Channel

4. Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release

5. Challenges and Opportunities for Therapeutics Targeting the Voltage-Gated Sodium Channel Isoform NaV1.7

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