PMID- 31129313
OWN - NLM
STAT- MEDLINE
DCOM- 20200513
LR  - 20200513
IS  - 1878-5832 (Electronic)
IS  - 1359-6446 (Linking)
VI  - 24
IP  - 7
DP  - 2019 Jul
TI  - Voltage-gated sodium channels: structures, functions, and molecular modeling.
PG  - 1389-1397
LID - S1359-6446(18)30448-3 [pii]
LID - 10.1016/j.drudis.2019.05.014 [doi]
AB  - 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.
CI  - Copyright (c) 2019 Elsevier Ltd. All rights reserved.
FAU - Xu, Lei
AU  - Xu L
AD  - Institute of Bioinformatics and Medical Engineering, School of Electrical and 
      Information Engineering, Jiangsu University of Technology, Changzhou 213001, 
      China.
FAU - Ding, Xiaoqin
AU  - Ding X
AD  - Beijing Institute of Pharmaceutical Chemistry, Beijing 102205, China.
FAU - Wang, Tianhu
AU  - Wang T
AD  - Institute of Bioinformatics and Medical Engineering, School of Electrical and 
      Information Engineering, Jiangsu University of Technology, Changzhou 213001, 
      China.
FAU - Mou, Shanzhi
AU  - Mou S
AD  - School of Mathematics and Physics, Jiangsu University of Technology, Changzhou 
      213001, China.
FAU - Sun, Huiyong
AU  - Sun H
AD  - Department of Medicinal Chemistry, School of Pharmacy, State Key Laboratory of 
      Natural Medicines, China Pharmaceutical University, Nanjing 210009, China. 
      Electronic address: huiyongsun@cpu.edu.cn.
FAU - Hou, Tingjun
AU  - Hou T
AD  - College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. 
      Electronic address: tingjunhou@zju.edu.cn.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20190523
PL  - England
TA  - Drug Discov Today
JT  - Drug discovery today
JID - 9604391
RN  - 0 (Voltage-Gated Sodium Channels)
SB  - IM
MH  - Animals
MH  - Binding Sites
MH  - Humans
MH  - Models, Molecular
MH  - Molecular Structure
MH  - Neuralgia
MH  - Voltage-Gated Sodium Channels/*chemistry/*physiology
EDAT- 2019/05/28 06:00
MHDA- 2020/05/14 06:00
CRDT- 2019/05/27 06:00
PHST- 2019/01/23 00:00 [received]
PHST- 2019/04/02 00:00 [revised]
PHST- 2019/05/17 00:00 [accepted]
PHST- 2019/05/28 06:00 [pubmed]
PHST- 2020/05/14 06:00 [medline]
PHST- 2019/05/27 06:00 [entrez]
AID - S1359-6446(18)30448-3 [pii]
AID - 10.1016/j.drudis.2019.05.014 [doi]
PST - ppublish
SO  - Drug Discov Today. 2019 Jul;24(7):1389-1397. doi: 10.1016/j.drudis.2019.05.014. 
      Epub 2019 May 23.