Crystal Structure of Lymnaea stagnalis AChBP Complexed with the Potent nAChR Antagonist DHβE Suggests a Unique Mode of Antagonism

A Shahsavar, JS Kastrup, EØ Nielsen, JL Kristensen… - 2012 - journals.plos.org
Nicotinic acetylcholine receptors (nAChRs) are pentameric ligand-gated ion channels that
belong to the Cys-loop receptor superfamily. These receptors are allosteric proteins that …

Lessons from nature: Structural studies and drug design driven by a homologous surrogate from invertebrates, AChBP

GA Camacho-Hernandez, P Taylor - Neuropharmacology, 2020 - Elsevier
It has been almost 20 years since the discovery and crystallization of a structural surrogate,
the Lymnaea stagnalis acetylcholine binding protein (Ls-AChBP), comprising the …

Galanthamine and non-competitive inhibitor binding to ACh-binding protein: evidence for a binding site on non-α-subunit interfaces of heteromeric neuronal nicotinic …

SB Hansen, P Taylor - Journal of molecular biology, 2007 - Elsevier
Rapid neurotransmission is mediated through a superfamily of Cys-loop receptors that
includes the nicotinic acetylcholine (nAChR), γ-aminobutyric acid (GABAA), serotonin (5 …

Atypical nicotinic agonist bound conformations conferring subtype selectivity

M Tomizawa, D Maltby, TT Talley… - Proceedings of the …, 2008 - National Acad Sciences
The nicotinic acetylcholine (ACh) receptor (nAChR) plays a crucial role in excitatory
neurotransmission and is an important target for drugs and insecticides. Diverse nAChR …

Structural and functional studies of the modulator NS9283 reveal agonist-like mechanism of action at α4β2 nicotinic acetylcholine receptors

JA Olsen, PK Ahring, JS Kastrup, M Gajhede… - Journal of Biological …, 2014 - ASBMB
Modulation of Cys loop receptor ion channels is a proven drug discovery strategy, but many
underlying mechanisms of the mode of action are poorly understood. We report the x-ray …

Gating of nicotinic ACh receptors; new insights into structural transitions triggered by agonist binding that induce channel opening

EA Gay, JL Yakel - The Journal of physiology, 2007 - Wiley Online Library
Nicotinic acetylcholine receptors (nAChRs) are in the superfamily of Cys‐loop ligand‐gated
ion channels, and are pentameric assemblies of five subunits, with each subunit arranged …

Structural characterization of agonist and antagonist-bound acetylcholine-binding protein from Aplysia californica

SB Hansen, G Sulzenbacher, T Huxford… - Journal of …, 2006 - search.proquest.com
Nicotinic acetylcholine receptors (nAChRs) are well-characterized allosteric transmembrane
proteins involved in the rapid gating of ions elicited by ACh. These receptors belong to the …

Crystal structure of acetylcholine-binding protein from Bulinus truncatus reveals the conserved structural scaffold and sites of variation in nicotinic acetylcholine …

PHN Celie, RV Klaassen… - Journal of Biological …, 2005 - ASBMB
The crystal structure of acetylcholine-binding protein (AChBP) from the mollusk Lymnaea
stagnalis is the established model for the ligand binding domains of the ligand-gated ion …

Gating of nicotinic ACh receptors: latest insights into ligand binding and function

JL Yakel - The Journal of Physiology, 2010 - Wiley Online Library
Nicotinic acetylcholine receptors (nAChRs) are in the superfamily of cys‐loop receptors, and
are widely expressed in the nervous system where they participate in a variety of …

Insight in nAChR subtype selectivity from AChBP crystal structures

P Rucktooa, AB Smit, TK Sixma - Biochemical pharmacology, 2009 - Elsevier
Nicotinic acetylcholine receptors (nAChRs) display a broad variety of subtypes, which in turn
present a complex subcellular and regional expression pattern in the brain, as well as a …