Differential interactions of closed, open, and desensitized states of the α7 nicotinic acetylcholine receptor with lipidic modulators

The α7 nicotinic acetylcholine receptor is a pentameric ligand-gated ion channel that critically modulates neuronal excitability, largely by importing Ca2+ ions. Similar to other channels in this family, agonist binding to the α7 receptor promotes the transition from a closed state to an open state, then rapidly to a desensitized state. Recent cryo-electron microscopy structures of the human α7 receptor in lipid nanodiscs were reported in multiple conformations, selectively stabilized by inhibitory, activating, or potentiating compounds.