Pannexin 1 Channels as a Therapeutic Target: Structure, Inhibition, and Outlook

被引:31
作者
Navis, Kathleen E. [1 ]
Fan, Churmy Y. [2 ]
Trang, Tuan [2 ]
Thompson, Roger J. [3 ]
Derksen, Darren J. [1 ]
机构
[1] Univ Calgary, Dept Chem, Calgary, AB T2N 1N4, Canada
[2] Univ Calgary, Hotchkiss Brain Inst, Dept Physiol & Pharmacol, Calgary, AB, Canada
[3] Univ Calgary, Dept Cell Biol & Anat, Hotchkiss Brain Inst, Calgary, AB T2N 4N1, Canada
来源
ACS CHEMICAL NEUROSCIENCE | 2020年 / 11卷 / 15期
基金
加拿大健康研究院; 加拿大自然科学与工程研究理事会;
关键词
Pannexin; 1; Channel; Structure; Pharmacology; Inhibition; Medicinal Chemistry; ATP RELEASE CHANNEL; FAMILY; ACTIVATION; CONNEXIN; PERMEABILITY; NEURONS; HEMICHANNELS; DYNAMICS; DEATH; CELLS;
D O I
10.1021/acschemneuro.0c00333
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Pannexin 1(Panx1) channels are transmembrarie proteins that release adenosine triphosphate and play an important role in intercellular communication. They are widely expressed in somatic and nervous system tissues, and their activity has been associated with many pathologies such as stroke, eiailepsy, inflammation, and chronic pain. 'While there are a variety of small molecules known to inhibit Panxl, currently little is known about the mechanism of channel inhibition, and there is a dearth of sufficiently potent and selective drugs targeting Panx1. Herein we provide a review of the current literature on P ara1 structural biology and knownpharmacological agents that will help provide a basis for rational development of Panx1 chemical modulators.
引用
收藏
页码:2163 / 2172
页数:10
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