Voets Thomas, Owsianik Grzegorz, Janssens Annelies, Talavera Karel, Nilius Bernd
Laboratory of Ion Channel Research, Division of Physiology, Department of Molecular Cell Biology, Campus Gasthuisberg O&N1, KU Leuven, Herestraat 49 bus 802, B-3000 Leuven, Belgium.
Nat Chem Biol. 2007 Mar;3(3):174-82. doi: 10.1038/nchembio862. Epub 2007 Feb 11.
TRPM8, a member of the transient receptor potential (TRP) channel superfamily, is expressed in thermosensitive neurons, in which it functions as a cold and menthol sensor. TRPM8 and most other temperature-sensitive TRP channels (thermoTRPs) are voltage gated; temperature and ligands regulate channel opening by shifting the voltage dependence of activation. The mechanisms and structures underlying gating of thermoTRPs are currently poorly understood. Here we show that charge-neutralizing mutations in transmembrane segment 4 (S4) and the S4-S5 linker of human TRPM8 reduce the channel's gating charge, which indicates that this region is part of the voltage sensor. Mutagenesis-induced changes in voltage sensitivity translated into altered thermal sensitivity, thereby establishing the strict coupling between voltage and temperature sensing. Specific mutations in this region also affected menthol affinity, which indicates a direct interaction between menthol and the TRPM8 voltage sensor. Based on these findings, we present a Monod-Wyman-Changeux-type model explaining the combined effects of voltage, temperature and menthol on TRPM8 gating.
瞬时受体电位(TRP)通道超家族成员TRPM8在热敏神经元中表达,在其中作为冷觉和薄荷醇感受器发挥作用。TRPM8和大多数其他温度敏感的TRP通道(热TRP通道)是电压门控的;温度和配体通过改变激活的电压依赖性来调节通道开放。目前对热TRP通道门控的机制和结构了解甚少。在此我们表明,人TRPM8跨膜片段4(S4)和S4 - S5连接区的电荷中和突变降低了通道的门控电荷,这表明该区域是电压感受器的一部分。诱变引起的电压敏感性变化转化为热敏感性改变,从而确立了电压和温度传感之间的严格耦合。该区域的特定突变也影响薄荷醇亲和力,这表明薄荷醇与TRPM8电压感受器之间存在直接相互作用。基于这些发现,我们提出了一个Monod - Wyman - Changeux型模型来解释电压、温度和薄荷醇对TRPM8门控的综合作用。
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