Navis Kathleen E, Fan Churmy Y, Trang Tuan, Thompson Roger J, Derksen Darren J
Department of Chemistry, University of Calgary, Calgary, Alberta T2N 1N4, Canada.
Department of Physiology and Pharmacology, Hotchkiss Brain Institute, University of Calgary, Calgary, Alberta T2N 4N1, Canada.
ACS Chem Neurosci. 2020 Aug 5;11(15):2163-2172. doi: 10.1021/acschemneuro.0c00333. Epub 2020 Jul 20.
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.
泛连接蛋白1（Panx1）通道是一种跨膜蛋白，可释放三磷酸腺苷，在细胞间通讯中发挥重要作用。它们广泛表达于躯体组织和神经系统组织中，其活性与许多病理状况相关，如中风、癫痫、炎症和慢性疼痛。虽然已知有多种小分子可抑制Panx1，但目前对通道抑制机制了解甚少，并且缺乏足够强效和选择性的靶向Panx1的药物。在此，我们综述了关于Panx1结构生物学和已知药理剂的当前文献，这将有助于为合理开发Panx1化学调节剂提供基础。
