[HTML][HTML] The α9α10 acetylcholine receptor: A non-neuronal nicotinic receptor

AB Elgoyhen - Pharmacological Research, 2023 - Elsevier
… This Cys-loop family includes the nicotinic acetylcholine receptors (nAChRs), serotonin type
3 receptors (5-… A (α9) 2 (α10) 3 stoichiometry has been determined for the rat recombinant …

Medicinal chemistry, pharmacology, and therapeutic potential of α-conotoxins antagonizing the α9α10 nicotinic acetylcholine receptor

X Li, HS Tae, Y Chu, T Jiang, DJ Adams… - Pharmacology & …, 2021 - Elsevier
… (A) Side sectional view of the α9α10 nAChR (brown and teal) structure embedded in the cell
membrane (blue). (B,C) Top view of the α9α10 nAChR structure in different stoichiometries. …

… NEURONAL NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS: FROM SUBTYPE SELECTIVE TO STOICHIOMETRIC ISOPHORM SELECTIVE PARTIAL …

R Appiani - 2023 - air.unimi.it
… This PhD thesis focuses on the study of the α4β2 nicotinic acetylcholine receptors (nAChRs).
This dissertation is divided into two parts. The first part is centred on the design, synthesis, …

Loss of choline agonism in the inner ear hair cell nicotinic acetylcholine receptor linked to the α10 subunit

MJ Moglie, I Marcovich, J Corradi… - Frontiers in molecular …, 2021 - frontiersin.org
… of α9α10 nAChRs to choline, the metabolite of acetylcholineα9α10 receptors it is a partial
agonist of the rat receptor. Making use of the expression of α9α10 heterologous receptors, …

Mechanism of Action and Structure–Activity Relationship of α-Conotoxin Mr1. 1 at the Human α9α10 Nicotinic Acetylcholine Receptor

J Liang, HS Tae, Z Zhao, X Li, J Zhang… - Journal of Medicinal …, 2022 - ACS Publications
α-Conotoxins (α-CTxs) can selectively target nicotinic acetylcholine receptors (nAChRs) and
are important drug leads for the treatment of cancer, chronic pain, and neuralgia. Here, we …

The α9α10 nicotinic acetylcholine receptor: a compelling drug target for hearing loss?

AB Elgoyhen - Expert opinion on therapeutic targets, 2022 - Taylor & Francis
… ear hair cell α9α10 nicotinic acetylcholine receptors (nAChRs) … The rational for targeting
this receptor is based on the fact … Alternate stoichiometries have been reported for this receptor

Dimerization of α-conotoxins as a strategy to enhance the inhibition of the human α7 and α9α10 nicotinic acetylcholine receptors

J Liang, HS Tae, X Xu, T Jiang… - Journal of Medicinal …, 2020 - ACS Publications
… Interestingly, in comparison to the monomer peptide, RgIA# dimer exhibited α9α10 subunit
stoichiometric-dependent sensitivity (Supporting Information, Figure S4 and Table S2). In our …

Selective agonists and antagonists of α9 versus α7 nicotinic acetylcholine receptors

RL Papke, H Andleeb, C Stokes, M Quadri… - ACS chemical …, 2022 - ACS Publications
… selective antagonists for either α7 or α9α10 receptors, respectively. While the downregulation
receptors with the subunit stoichiometry α4(2)β2(3), (34) low sensitivity α4β2 (α4(3)β2(2)) …

Hair cell α9α10 nicotinic acetylcholine receptor functional expression regulated by ligand binding and deafness gene products

S Gu, D Knowland, JA Matta… - Proceedings of the …, 2020 - National Acad Sciences
… synapse involves α9α10 nicotinic acetylcholine receptors (… assembly and surface expression
of α9α10 require ligand binding. … postsynaptic α9α10 function and abnormally retain α9α10-…

Discovery and Structural and Functional Characterization of a Novel A-Superfamily Conotoxin Targeting α9α10 Nicotinic Acetylcholine Receptor

Q Huang, X Chu, H Zhang, S Yu, L Zhang… - ACS Chemical …, 2022 - ACS Publications
α9α10 nAChRs and a new motif for designing potent inhibitors against α9α10 nAChRs. …
This work provides a novel conotoxin potently targeting α9α10 nAChRs and a new motif to …