Vandenberg, Jamie I and Perozo, Eduardo and Allen, Toby W (2017) Towards a Structural View of Drug Binding to hERG K(+) Channels. Trends in Pharmacological Sciences, 38 (10). pp.899-907. ISSN 1873-3735 (PP OA)
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Abstract
The human ether-a-go-go-related gene (hERG) K(+) channel is of great medical and pharmaceutical relevance. Inherited mutations in hERG result in congenital long-QT syndrome which is associated with a markedly increased risk of cardiac arrhythmia and sudden death. hERG K(+) channels are also remarkably susceptible to block by a wide range of drugs, which in turn can cause drug-induced long-QT syndrome and an increased risk of sudden death. The recent determination of the near-atomic resolution structure of the hERG K(+) channel, using single-particle cryo-electron microscopy (cryo-EM), provides tremendous insights into how these channels work. It also suggests a way forward in our quest to understand why these channels are so promiscuous with respect to drug binding.
| Item Type: | Article |
|---|---|
| Subjects: | R Medicine > R Medicine (General) |
| Depositing User: | Repository Administrator |
| Date Deposited: | 20 Jul 2017 05:40 |
| Last Modified: | 13 Dec 2018 02:42 |
| URI: | https://eprints.victorchang.edu.au/id/eprint/604 |
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