Recent Insight into Lipid Binding and Lipid Modulation of Pentameric Ligand-Gated Ion Channels

Pentameric ligand-gated ion channels (pLGICs) play a leading role in synaptic communication, are implicated in a variety of neurological processes, and are important targets for the treatment of neurological and neuromuscular disorders. Endogenous lipids and lipophilic compounds are potent modulators of pLGIC function and may help shape synaptic communication. Increasing structural and biophysical data reveal sites for lipid binding to pLGICs. Here, we update our evolving understanding of pLGIC-lipid interactions highlighting newly identified modes of lipid binding along with the mechanistic understanding derived from the new structural data.

Automated summary

Pentameric ligand-gated ion channels (pLGICs) play a crucial role in synaptic communication and are considered important targets for treating neurological disorders. Lipids and lipophilic compounds modulate pLGIC function, and recent structural and biophysical data have identified binding sites for lipids on pLGICs.