Dyclonine inhibition of TRPV3: from functional discovery to structural insight
Dyclonine inhibition of TRPV3: from functional discovery to structural insight
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TRPV3 的达克罗宁抑制：从功能发现到结构洞察
DOI：
10.1016/j.ceca.2022.102617
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发表时间：
2022
期刊：
影响因子：
4
通讯作者：
Jing Yao
中科院分区：
文献类型：
--
作者：
Peiyu Wang;Xiaoyi Mo;Dongdong Li;Jing Yao
Yao和同事最近报道了临床批准的局麻药dyclonine作为TRPV3的有效抑制剂，并在TRPV3孔区发现了几个可以改变抑制效率的关键残基。Neuberger等人的研究揭示了TRPV3-dyclonine复合物的低温电子显微镜（cryo-EM）图谱，揭示了抑制剂在通道孔内的结合。地克隆碱的变构结合位点成为设计trpv3靶向药物的潜在可利用模板。
• Yao and colleagues recently reported that the clinically approved local anesthetic dyclonine acts as a potent inhibitor of TRPV3, and identified several key residues in TRPV3 pore region that could toggle the inhibitory efficiency. The study by Neuberger et al. sheds light on the cryo-electron microscopy (cryo-EM) map of TRPV3–dyclonine complex, which reveals binding of the inhibitor within the channel pore. The allosteric binding site of dyclonine emerges as a potentially leverageable template for designing TRPV3-targeting drugs.