低温电镜揭示 TRPA1 的致刺激机制。
Insights into the Irritating Mechanisms of TRPA1 Revealed by Cryo-EM.
机构信息
Department of Molecular Genetics, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
Department of Molecular Genetics, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA; Department of Biophysics, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.
出版信息
Neuron. 2021 Jan 20;109(2):194-196. doi: 10.1016/j.neuron.2020.12.017.
TRPA1 is a promising target for the development of novel treatments for chronic pain. In this issue of Neuron, Liu et al. (2021) report a novel non-covalent TRPA1-biased agonist, GNE551, revealing a unique binding pocket by cryo-EM and activation properties that pave a path toward new avenues in the treatment of chronic pain.
TRPA1 是开发新型慢性疼痛治疗药物的有前途的靶点。在本期《神经元》杂志上，Liu 等人（2021）报告了一种新型非共价的 TRPA1 偏向激动剂 GNE551，通过低温电镜揭示了一个独特的结合口袋和激活特性，为慢性疼痛的治疗开辟了新途径。
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