向下抑制：TPC2 中 VSD II 受拮抗剂诱导的向下移位。
Descending to inhibit: Antagonist-induced downward shift of VSD II in TPC2.
机构信息
Division of Biophysics and Neurobiology, Department of Molecular and Cellular Physiology, National Institute for Physiological Sciences, Okazaki, Aichi, Japan; Department of Physiological Sciences, School of Life Science, The Graduate University for Advanced Studies (SOKENDAI), Hayama, Kanagawa, Japan.
出版信息
Structure. 2024 Aug 8;32(8):1025-1027. doi: 10.1016/j.str.2024.07.005.
In this issue of Structure, Chi et al. report structural and functional studies that reveal the inhibition mechanism of the lysosomal two-pore channel TPC2 by the antagonist SG-094, which is of interest for drug development. Antagonist binding induces the downward displacement of the voltage-sensor domain II (VSD II), which is accompanied by asymmetric conformational rearrangements of the entire channel.
在本期《结构》杂志中，Chi 等人报告了结构和功能研究，揭示了溶酶体双孔通道 TPC2 被拮抗剂 SG-094 抑制的机制，这对于药物开发具有重要意义。拮抗剂结合诱导电压传感器域 II（VSD II）向下位移，同时整个通道发生不对称构象重排。
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