Crystal structure of a human neuronal nAChR extracellular domain in pentameric assembly: Ligand-bound α2 homopentamer
Copyright policy )Crystal structure of a human neuronal nAChR extracellular domain in pentameric assembly: Ligand-bound α2 homopentamer
Significance Nicotinic acetylcholine receptors (nAChRs) are pentameric ligand-gated ion channels involved in fast neurotransmission. Here, we present the crystal structure of the homopentameric assembly of the extracellular domain (ECD) of α2 nAChR subunit in complex with an agonist. The structure provides a unique opportunity to probe the interactions involved in the formation of the ligand binding site of a WT nAChR and their role in stabilizing an agonist. Furthermore, functional studies revealed the role of additional residues in the activation and desensitization of the α2β2 nAChRs. High sequence identity of α2 ECD with other neuronal subunits signifies the importance of the structure as a template for modeling several neuronal nAChR ECDs and for designing nAChR subtype-specific drugs against related diseases.
- Pasteur Hellenic Institute Greece
- Institut Pasteur France
- National and Kapodistrian University of Athens Greece
- Eginition Hospital Greece
- University of Patras Greece
Models, Molecular, Protein Conformation, alpha-Helical, Binding Sites, Patch-Clamp Techniques, Amino Acid Motifs, Gene Expression, Bridged Bicyclo Compounds, Heterocyclic, Crystallography, X-Ray, Pichia, Protein Subunits, Mutation, Oocytes, Animals, Humans, Female, Protein Conformation, beta-Strand, Protein Interaction Domains and Motifs, Cloning, Molecular, Protein Multimerization, Protein Binding
Models, Molecular, Protein Conformation, alpha-Helical, Binding Sites, Patch-Clamp Techniques, Amino Acid Motifs, Gene Expression, Bridged Bicyclo Compounds, Heterocyclic, Crystallography, X-Ray, Pichia, Protein Subunits, Mutation, Oocytes, Animals, Humans, Female, Protein Conformation, beta-Strand, Protein Interaction Domains and Motifs, Cloning, Molecular, Protein Multimerization, Protein Binding
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