Allosteric modulation of nicotinic acetylcholine receptors

A Chatzidaki, NS Millar - Biochemical pharmacology, 2015 - Elsevier
Nicotinic acetylcholine receptors (nAChRs) are receptors for the neurotransmitter
acetylcholine and are members of the 'Cys-loop'family of pentameric ligand-gated ion …

Allosteric modulation of nicotinic acetylcholine receptors

D Bertrand, M Gopalakrishnan - Biochemical pharmacology, 2007 - Elsevier
Allosteric modulation refers to the concept that proteins could exist in multiple
conformational states and that binding of allosteric ligands alters the energy barriers or …

Allosteric modulations of the nicotinic acetylcholine receptor

C Léna, JP Changeux - Trends in neurosciences, 1993 - cell.com
The nicotinic acetylcholine receptor behaves as an allosteric protein with multiple,
interconvertible conformations: a resting state, an open channel state and several …

[HTML][HTML] Advances in small molecule selective ligands for heteromeric nicotinic acetylcholine receptors

C Matera, C Papotto, C Dallanoce… - Pharmacological Research, 2023 - Elsevier
The study of nicotinic acetylcholine receptors (nAChRs) has significantly progressed in the
last decade, due to a) the improved techniques available for structural studies; b) the …

Allosteric modulators of the α7 nicotinic acetylcholine receptor

R Faghih, M Gopalakrishnan… - Journal of medicinal …, 2008 - ACS Publications
Ion channels expressed in the plasma membrane are broadly classified as voltage-gated
ion channels (VGICa) or ligand-gated ion channels (LGIC) where the ligand usually is …

Agonist activation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site

JKK Gill, M Savolainen, GT Young… - Proceedings of the …, 2011 - National Acad Sciences
Conventional nicotinic acetylcholine receptor (nAChR) agonists, such as acetylcholine, act
at an extracellular “orthosteric” binding site located at the interface between two adjacent …

[HTML][HTML] Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects

JKK Gill-Thind, P Dhankher, JM D'Oyley… - Journal of Biological …, 2015 - ASBMB
Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of
agonists such as acetylcholine to an extracellular site that is located at the interface between …

Design of ligands for the nicotinic acetylcholine receptors: the quest for selectivity

WH Bunnelle, M MJ Dart… - Current Topics in …, 2004 - ingentaconnect.com
In the last decade, nicotinic acetylcholine receptors (nAChRs) have emerged as important
targets for drug discovery. The therapeutic potential of nicotinic agonists depends …

Introductory lecture: allosteric modulation of Torpedo nicotinic acetylcholine receptor Ion Channel activity by noncompetitive agonists

A Maelicke, T Coban, A Storch… - Journal of Receptors …, 1997 - Taylor & Francis
Similar to other neuroreceptors of the vertebrate central nervous system, the nicotinic
acetylcholine receptor (nAChR) is subject to modulatory control by allosterically acting …

Orthosteric and allosteric potentiation of heteromeric neuronal nicotinic acetylcholine receptors

J Wang, J Lindstrom - British journal of pharmacology, 2018 - Wiley Online Library
Heteromeric nicotinic ACh receptors (nAChRs) were thought to have two orthodox agonist‐
binding sites at two α/β subunit interfaces. Highly selective ligands are hard to develop by …