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 …
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 …
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 …
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 …
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
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 …
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** …
Here, we present the discovery of a novel class of benzimidazole-based allosteric
modulators of nicotinic acetylcholine receptors (nAChRs). The modulators were developed …
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 …
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
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 …
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 …
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 …
involved in regulating neurotransmission in the central nervous system (CNS) by conducting …