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Pannexin 1 Channels as a Therapeutic Target: Structure, Inhibition, and Outlook.
ACS Chemical Neuroscience ( IF 4.1 ) Pub Date : 2020-07-08 , DOI: 10.1021/acschemneuro.0c00333
Kathleen E Navis 1 , Churmy Y Fan 2 , Tuan Trang 2 , Roger J Thompson 3 , Darren J Derksen 1
Affiliation  

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.

中文翻译:

Pannexin 1 通道作为治疗目标:结构、抑制和前景。

Pannexin 1 (Panx1) 通道是释放三磷酸腺苷的跨膜蛋白,在细胞间通讯中起重要作用。它们在躯体和神经系统组织中广泛表达,它们的活性与许多疾病有关,例如中风、癫痫、炎症和慢性疼痛。虽然已知有多种小分子可以抑制 Panx1,但目前对通道抑制的机制知之甚少,并且缺乏足够有效和选择性的靶向 Panx1 的药物。在这里,我们回顾了当前有关 Panx1 结构生物学和已知药理剂的文献,这将有助于为 Panx1 化学调节剂的合理开发提供基础。
更新日期:2020-08-05
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