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Papers of the Week

Papers: 25 May 2019 - 31 May 2019

Pharmacology/Drug Development

2019 Jul

Drug Discov Today



Voltage-gated sodium channels: structures, functions, and molecular modeling.


Xu L, Ding X, Wang T, Mou S, Sun H, Hou T
Drug Discov Today. 2019 Jul; 24(7):1389-1397.
PMID: 31129313.


Voltage-gated sodium channels (VGSCs), formed by 24 transmembrane segments arranged into four domains, have a key role in the initiation and propagation of electrical signaling in excitable cells. VGSCs are involved in a variety of diseases, including epilepsy, cardiac arrhythmias, and neuropathic pain, and, therefore, have been regarded as appealing therapeutic targets for the development of anticonvulsant, antiarrhythmic, and local anesthetic drugs. In this review, we discuss recent advances in understanding the structures and biological functions of VGSCs. In addition, we systematically summarize eight pharmacologically distinct ligand-binding sites in VGSCs and representative isoform-selective VGSC modulators in clinical trials. Finally, we review studies on molecular modeling and computer-aided drug design (CADD) for VGSCs to help understanding of biological processes involving VGSCs.