Department of Physiological Sciences, SOKENDAI, Okazaki, Japan.
Division of Cell Signaling, National Institute for Physiological Sciences, Okazaki, Japan.
Commun Biol. 2021 Mar 5;4(1):293. doi: 10.1038/s42003-021-01776-0.
Monoterpenes are major constituents of plant-derived essential oils and have long been widely used for therapeutic and cosmetic applications. The monoterpenes menthol and camphor are agonists or antagonists for several TRP channels such as TRPM8, TRPV1, TRPV3 and TRPA1. However, which regions within TRPV1 and TRPV3 confer sensitivity to monoterpenes or other synthesized chemicals such as 2-APB are unclear. In this study we identified conserved arginine and glycine residues in the linker between S4 and S5 that are related to the action of these chemicals and validated these findings in molecular dynamics simulations. The involvement of these amino acids differed between TRPV3 and TRPV1 for chemical-induced and heat-evoked activation. These findings provide the basis for characterization of physiological function and biophysical properties of ion channels.
单萜是植物源性精油的主要成分，长期以来一直广泛用于治疗和美容应用。薄荷醇和樟脑是几种 TRP 通道（如 TRPM8、TRPV1、TRPV3 和 TRPA1）的激动剂或拮抗剂。然而，TRPV1 和 TRPV3 中的哪些区域对单萜或其他合成化学物质（如 2-APB）敏感尚不清楚。在这项研究中，我们确定了 S4 和 S5 之间连接环中与这些化学物质作用相关的保守精氨酸和甘氨酸残基，并在分子动力学模拟中验证了这些发现。这些氨基酸在化学诱导和热激激活中在 TRPV3 和 TRPV1 之间的参与方式不同。这些发现为离子通道的生理功能和生物物理特性的表征提供了基础。
