Progress in nicotinic receptor structural biology

• Published in: Neuropharmacology Vol. 171; p. 108086
• Main Authors: Gharpure, Anant, Noviello, Colleen M., Hibbs, Ryan E.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-07-2020
• Subjects: Cryo-EM; Nicotine; Nicotinic acetylcholine receptor; Structural biology; Cryo-EM; Structural biology; Nicotinic acetylcholine receptor; Nicotine
• ISSN: 0028-3908; 1873-7064
• DOI: 10.1016/j.neuropharm.2020.108086

Here we begin by briefly reviewing landmark structural studies on the nicotinic acetylcholine receptor. We highlight challenges that had to be overcome to push through resolution barriers, then focus on what has been gleaned in the past few years from crystallographic and single particle cryo-EM studies of different nicotinic receptor subunit assemblies and ligand complexes. We discuss insights into ligand recognition, ion permeation, and allosteric gating. We then highlight some foundational aspects of nicotinic receptor structural biology that remain unresolved and are areas ripe for future exploration.
This article is part of the special issue on ‘Contemporary Advances in Nicotine Neuropharmacology’.