Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations

DK Williams, J Wang, RL Papke - Biochemical pharmacology, 2011 - Elsevier
Neuronal nicotinic acetylcholine receptors (nAChR), recognized targets for drug
development in cognitive and neuro-degenerative disorders, are allosteric proteins with …

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 …

Augmentation of cognitive function by NS9283, a stoichiometry‐dependent positive allosteric modulator of α2‐and α4‐containing nicotinic acetylcholine receptors

DB Timmermann, K Sandager‐Nielsen… - British journal of …, 2012 - Wiley Online Library
BACKGROUND AND PURPOSE Positive allosteric modulation of α4β2 nicotinic
acetylcholine (nACh) receptors could add a new dimension to the pharmacology and …

Drug development in channelopathies: Allosteric modulation of ligand-gated and voltage-gated ion channels

Y Zhang, K Wang, Z Yu - Journal of medicinal chemistry, 2020 - ACS Publications
Ion channels have been characterized as promising drug targets for treatment of numerous
human diseases. Functions of ion channels can be fine-tuned by allosteric modulators …

Rabies virus modifies host behaviour through a snake-toxin like region of its glycoprotein that inhibits neurotransmitter receptors in the CNS

K Hueffer, S Khatri, S Rideout, MB Harris, RL Papke… - Scientific reports, 2017 - nature.com
Rabies virus induces drastic behaviour modifications in infected hosts. The mechanisms
used to achieve these changes in the host are not known. The main finding of this study is …

Discovery of a Novel Class of Benzimidazole-Based Nicotinic Acetylcholine Receptor Modulators: Positive and Negative Modulation Arising from Overlap** …

L Zhou, V Dau, AA Jensen - Journal of Medicinal Chemistry, 2023 - ACS Publications
Here, we present the discovery of a novel class of benzimidazole-based allosteric
modulators of nicotinic acetylcholine receptors (nAChRs). The modulators were developed …

Positive and negative modulation of nicotinic receptors

HR Arias - Advances in protein chemistry and structural biology, 2010 - Elsevier
Nicotinic acetylcholine receptors (AChRs) are one of the best characterized ion channels
from the Cys-loop receptor superfamily. The study of acetylcholine binding proteins and …

Advances in the In vitro and In vivo pharmacology of Alpha4beta2 nicotinic receptor positive allosteric modulators

JL Wilkerson, F Deba, ML Crowley, AK Hamouda… - …, 2020 - Elsevier
Receptors containing α4 and β2 subunits are a major neuronal nicotinic acetylcholine
receptor (nAChR) subtype in the brain. This receptor plays a critical role in nicotine …

Recent progress in neuroactive marine natural products

R Sakai, GT Swanson - Natural product reports, 2014 - pubs.rsc.org
Covering: 1995 to early 2013 This review covers the isolation, chemical structure, biological
activity, structure activity relationships including synthesis of chemical probes, and …

Targeting α4β2 nicotinic acetylcholine receptors in central nervous system disorders: perspectives on positive allosteric modulation as a therapeutic approach

M Grupe, M Grunnet, JF Bastlund… - Basic & clinical …, 2015 - Wiley Online Library
The nicotinic acetylcholine receptors (nAChR s) are ligand‐gated ion channels broadly
involved in regulating neurotransmission in the central nervous system (CNS) by conducting …