Pannexin 1 Channels as a Therapeutic Target: Structure, Inhibition, and Outlook
Date
2020-01
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Abstract
Pannexin 1 (Panx1) channels are transmembrane 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, epilepsy, inflammation, and chronic pain. While there are a variety of small molecules known to inhibit Panx1, 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 Panx1 structural biology and known pharmacological agents that will help provide a basis for rational development of Panx1 chemical modulators.
Description
Funding for this research was provided through a Queen Elizabeth II Graduate Research Scholarship, Alberta Graduate Excellence Scholarship (AGES), Natural Sciences and Engineering Research Council (NSERC), CIHR (Canadian Institutes of Health Research), and the Alberta Children’s Hospital Foundation and Research Institute.
Keywords
Pannexin 1, Pharmacology, Inhibition, Medicinal Chemistry, Channel, Structure
Citation
Navis, K. E., Fan, C. Y., Trang, T., Thompson, R. J., & Derksen, D. J. (2020). Pannexin 1 channels as a therapeutic target: Structure, inhibition, and outlook. ACS Chemical Neuroscience, 11(15), 2163-2172.