Recent progress in sodium channel modulators for pain

被引：140

作者：

Bagal, Sharan K. ^{[1
]}

Chapman, Mark L. ^{[2
]}

Marron, Brian E. ^{[3
]}

Prime, Rebecca ^{[4
]}

Storer, R. Ian ^{[1
]}

Swain, Nigel A. ^{[1
]}

机构：

[1] Pfizer Neusentis, Worldwide Med Chem, Cambridge CB21 6GS, England

[2] Pfizer Neusentis, Electrophysiology, Durham, NC USA

[3] Pfizer Neusentis, Chemistry, Durham, NC USA

[4] Pfizer Neusentis, Electrophysiology, Cambridge CB21 6GS, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 16期

关键词：

Voltage-gated sodium channels; Electrophysiology screening; Sodium channel toxins; Sodium channel structure; Sodium channel drugs; OF-FUNCTION MUTATIONS; HUWENTOXIN-IV; CRYSTAL-STRUCTURE; DRUG DISCOVERY; NA+ CURRENT; PROTX-II; INHIBITOR; TETRODOTOXIN; MECHANISMS; POTENT;

D O I：

10.1016/j.bmcl.2014.06.038

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Voltage-gated sodium channels (Na(v)s) are an important family of transmembrane ion channel proteins and Na-v drug discovery is an exciting field. Pharmaceutical investment in Navs for pain therapeutics has expanded exponentially due to genetic data such as SCN10A mutations and an improved ability to establish an effective screen sequence for example IonWorks Barracuda (R), Synchropatch (R) and Qube (R). Moreover, emerging clinical data (AZD-3161, XEN402, CNV1014802, PF-05089771, PF-04531083) combined with recent breakthroughs in Nav structural biology pave the way for a future of fruitful prospective Nav drug discovery. (C) 2014 The Authors. Published by Elsevier Ltd.

引用

页码：3690 / 3699

页数：10

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