Recent progress in sodium channel modulators for pain

Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav 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 e...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2014-08, Vol.24 (16), p.3690-3699
Hauptverfasser:	Bagal, Sharan K., Chapman, Mark L., Marron, Brian E., Prime, Rebecca, Storer, R. Ian, Swain, Nigel A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Drug Discovery Electrophysiology screening Humans Pain - drug therapy Sodium Channel Blockers - chemistry Sodium Channel Blockers - pharmacology Sodium Channel Blockers - therapeutic use Sodium channel drugs Sodium channel structure Sodium channel toxins Voltage-gated sodium channels Voltage-Gated Sodium Channels - chemistry Voltage-Gated Sodium Channels - metabolism
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Beschreibung
Zusammenfassung:	Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav 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®, Synchropatch® and Qube®. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2014.06.038