Human α10 nicotinic acetylcholine receptor subunits assemble to form functional receptors

Journal of Biological Chemistry, Год журнала: 2025, Номер unknown, С. 108182 - 108182

Опубликована: Янв. 1, 2025

Nicotinic acetylcholine receptors (nAChRs) are pentameric ligand-gated ion channels. In mammals, there 16 individual nAChR subunits allowing for numerous possible heteromeric compositions. nAChRs assembled from α7 or α9 will form as homopentamers. contrast, the structurally related α10 subunit has historically been thought to require function. Recently, however, strychnine was shown enable expression of human in Xenopus laevis oocytes mammalian cells, prompting a re-examination whether can self-assemble absence strychnine. present study, acetylcholine-evoked ionic currents were obtained by co-expression with transmembrane protein resistance inhibitors cholinesterase-3 (RIC-3) oocytes. Furthermore, creation gain-of-function reporter mutation, V13'T, second domain demonstrated that presence RIC-3. The antagonist sensitivity homomeric is distinct closely and α9α10 subtypes. homomers blocked α-bungarotoxin but insensitive α-conotoxin [V11L;V16D]ArIB RgIA-5474, which potently block nAChRs, respectively. These studies yield insight into assembly functional provide tools development -nAChR-selective ligands.

Язык: Английский

Special Issue "The multifaceted activities of nervous and non-nervous neuronal nicotinic acetylcholine receptors in physiology and pathology"

Pharmacological Research, Год журнала: 2024, Номер 205, С. 107239 - 107239

Опубликована: Май 25, 2024

Язык: Английский