Small molecule inhibits KCNQ channels with a non-blocking
2025年1月15日 · Guided by cryogenic electron microscopy, patch-clamp recordings and molecular dynamics simulations, we reveal that Ebio3 attaches to the outside of the inner gate, …
A small-molecule activation mechanism that directly opens the KCNQ2 …
2024年1月2日 · Through structure-based virtual screening, we identified a new scaffold compound, Ebio1, serving as a potent and subtype-selective activator for the voltage-gated …
Molecular basis for ligand activation of the human KCNQ2 channel
2020年9月3日 · All of the four mutations we tested, W236A, F240A, L299A and S303A, decreased the potentiation activity of RTG on KCNQ2 by preventing or attenuating the left-shift …
The CBD-bound KCNQ2-CaM structure (KCNQ2-CaMCBD) a The …
Here we report cryo-electron microscopy (cryo-EM) structures of human KCNQ2-CaM in complex with three acti...
The HN37-bound KCNQ2-CaM structure (KCNQ2-CaMHN37) a …
KCNQ2 can be activated by analgesics and antiepileptic drugs but their activation mechanisms remain unclear. Here we report cryo-electron microscopy (cryo-EM) structures of human …
重大进展！Cell子刊揭示配体激活人源KCNQ2通道的分子基础 - 知乎
该文章利用 冷冻电镜技术 解析了人源 KCNQ2 及其与小分子 RTG 和 ztz240 （一种 ICA-27243 结构类似物）的结构，揭示了配体激活人源 KCNQ2 通道的分子基础。 Fig 1. 文章截图. 作者首 …
The conductance of KCNQ2 and its pathogenic variants is
2025年3月5日 · KCNQ2 channel subunits form part of the M-current and underlie one of the major potassium currents throughout the human nervous system, regulating resting membrane …
Ligand activation mechanisms of human KCNQ2 channel
2023年10月19日 · Here we report cryo-electron microscopy (cryo-EM) structures of human KCNQ2-CaM in complex with three activators, namely the antiepileptic drug cannabidiol …
项目推介 | 新一代KCNQ2/3激动剂的开发
2024年12月13日 · kcnq2和kcnq3形成同源或异源四聚体通道，是形成神经元m电流的主要分子基础。 KCNQ2和KCNQ3突变导致神经元过度兴奋和癫痫发作的发生，被认为是下一代抗癫痫药 …
Ligand activation mechanisms of human KCNQ2 channel - PMC
Here we report cryo-electron microscopy (cryo-EM) structures of human KCNQ2-CaM in complex with three activators, namely the antiepileptic drug cannabidiol (CBD), the lipid …