Structural basis for promiscuous action of monoterpenes on TRP channels

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. Thi Hong Dung Nguyen et al. identify which regions within TRP channels TRPV1 and TRPV3 confer their sensitivity to monoterpenes that are major constituents of plant-derived essential oils. This study provides insights into how different TRP channels respond to chemical or heat stimuli.

Automated summary

The study identified specific regions within TRPV1 and TRPV3 that confer sensitivity to monoterpenes and validated these findings through molecular dynamics simulations. The involvement of these amino acids differs between different TRP channels, revealing insights into how different TRP channels respond to chemical or heat stimuli.