期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 16, 页码 3690-3699出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.06.038
关键词
Voltage-gated sodium channels; Electrophysiology screening; Sodium channel toxins; Sodium channel structure; Sodium channel drugs
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.
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