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Mechanisms and energetics of potassium channel block by local anesthetics and antifungal agents

Chen, Rong; Gryn'ova, Ganna; Wu, Yingliang; Coote, Michelle; Chung, Shin-Ho


Many drug molecules inhibit the conduction of several families of cation channels by binding to a small cavity just below the selectivity filter of the channel protein. The exact mechanisms governing drug-channel binding and the subsequent inhibition of conduction are not well understood. Here the inhibition of two K+channel isoforms, Kv1.2 and KCa3.1, by two drug molecules, lidocaine and TRAM-34, is examined in atomic detail using molecular dynamics simulations. A conserved...[Show more]

CollectionsANU Research Publications
Date published: 2014
Type: Journal article
Source: Biochemistry
DOI: 10.1021/bi5009408


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