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Rhodojaponin Ⅵ indirectly targets Cav2.2 channels via N-ethylmaleimide-sensitive fusion protein to alleviate neuropathic pain

查看全文 作　　者：Keliang [1]Chen;Tao [2]Wang;Yong [1]Li;Jun [1]Wu;Cheng-Xiao [1]Zhao;Sheng [1]Liu;Fengrun [2]Sun;Yehong [2]Fang;Jiahuan [1]Hu;Jinping [1]Hu;Chong-Jing [1]Zhang;Haibo [1]Yu;Chao [2]Ma;Shi-Shan [1]Yu 高影响力作者 机构地区：[1]State Key Laboratory of Bioactive Substance and Function of Natural Medicines,Institute of Materia Medica,Chinese Academy of Medical Sciences and Peking Union Medical College,Beijing 100050,China;[2]Institute of Basic Medical Sciences,Neuroscience Center,Chinese Academy of Medical Sciences,Department of Human Anatomy,Histology and Embryology,School of Basic Medicine,Peking Union Medical College,Beijing 100005,China高影响力机构 出　　处：《Acta Pharmaceutica Sinica B》索引2023年第13卷第3期,共11页高影响力期刊 基　　金：The Natural Science Foundation of China (Nos.21732008,and 81771205);CAMS Innovation Fund for Medical Sciences (CIFMS,Nos.CIFMS-2022-I2M-JB-009,China);The National Postdoctoral Program for Innovative Talents (No.BX20180053,China) 摘　　要：Neuropathic pain is a chronic disease that severely afflicts the life and emotional status of patients,but currently available treatments are often ineffective.Novel therapeutic targets for the alleviation of neuropathic pain are urgently needed.Rhodojaponin Ⅵ,a grayanotoxin from Rhododendron molle,showed remarkable antinociceptive efficacy in models of neuropathic pain,but its biotargets and mechanisms are unknown.Given the reversible action of rhodojaponin Ⅵ and the narrow range over which its structure can be modified,we perforwmed thermal proteome profiling of the rat dorsal root ganglion to determine the protein target of rhodojaponin Ⅵ.N-Ethylmaleimide-sensitive fusion(NSF) was confirmed as the key target of rhodojaponin Ⅵ through biological and biophysical experiments.Functional validation showed for the first time that NSF facilitated trafficking of the Cav2.2 channel to induce an increase in Ca2+current intensity,whereas rhodojaponin Ⅵ reversed the effects of NSF.In conclusion,rhodojaponin Ⅵ represents a unique class of analgesic natural products targeting Cav2.2 channels via NSF. 关 键 词：Natural product Rhodojaponin VI Neuropathic pain NSF Cav2.2
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