[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 …
agonists such as acetylcholine to an extracellular site that is located at the interface between …
[HTML][HTML] The influence of allosteric modulators and transmembrane mutations on desensitisation and activation of α7 nicotinic acetylcholine receptors
A Chatzidaki, JM D'Oyley, JKK Gill-Thind… - …, 2015 - Elsevier
Acetylcholine activates nicotinic acetylcholine receptors (nAChRs) by binding at an extracellular
orthosteric site. Previous studies have described several positive allosteric modulators (…
orthosteric site. Previous studies have described several positive allosteric modulators (…
Differential contribution of subunit interfaces to α9α10 nicotinic acetylcholine receptor function
Nicotinic acetylcholine receptors can be assembled from either homomeric or heteromeric
pentameric subunit combinations. At the interface of the extracellular domains of adjacent …
pentameric subunit combinations. At the interface of the extracellular domains of adjacent …
[HTML][HTML] Identification by virtual screening and functional characterisation of novel positive and negative allosteric modulators of the α7 nicotinic acetylcholine receptor
CLC Smelt, VR Sanders, J Newcombe, RP Burt… - …, 2018 - Elsevier
Several previous studies have demonstrated that the activity of neurotransmitters acting on
ligand-gated ion channels such as the nicotinic acetylcholine receptor (nAChR) can be …
ligand-gated ion channels such as the nicotinic acetylcholine receptor (nAChR) can be …
[HTML][HTML] Critical molecular determinants of α7 nicotinic acetylcholine receptor allosteric activation: separation of direct allosteric activation and positive allosteric …
NA Horenstein, RL Papke, AR Kulkarni… - Journal of Biological …, 2016 - ASBMB
The α7 nicotinic acetylcholine receptors (nAChRs) are uniquely sensitive to selective positive
allosteric modulators (PAMs), which increase the efficiency of channel activation to a level …
allosteric modulators (PAMs), which increase the efficiency of channel activation to a level …
Differing activity profiles of the stereoisomers of 2, 3, 5, 6TMP-TQS, a putative silent allosteric modulator of α7 nAChR
RL Papke, S Garai, C Stokes, NA Horenstein… - Molecular …, 2020 - ASPET
Many synthetic compounds to which we attribute specific activities are produced as racemic
mixtures of stereoisomers, and it may be that all the desired activity comes from a single …
mixtures of stereoisomers, and it may be that all the desired activity comes from a single …
[HTML][HTML] An accessory agonist binding site promotes activation of α4β2* nicotinic acetylcholine receptors
J Wang, A Kuryatov, A Sriram, Z Jin… - Journal of Biological …, 2015 - ASBMB
Neuronal nicotinic acetylcholine receptors containing α4, β2, and sometimes other subunits
(α4β2* nAChRs) regulate addictive and other behavioral effects of nicotine. These nAChRs …
(α4β2* nAChRs) regulate addictive and other behavioral effects of nicotine. These nAChRs …
Discovery of BNC375, a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs
AJ Harvey, TD Avery, L Schaeffer… - ACS Medicinal …, 2019 - ACS Publications
… For example, in the work reported by Gill-Thind, (14) the cis–cis diastereomers were all
classified as allosteric agonists or Type II PAMs. In contrast, all of the cis–trans diastereomers …
classified as allosteric agonists or Type II PAMs. In contrast, all of the cis–trans diastereomers …
Diversity of nicotinic acetylcholine receptor positive allosteric modulators revealed by mutagenesis and a revised structural model
J Newcombe, A Chatzidaki, TD Sheppard, M Topf… - Molecular …, 2018 - ASPET
By combining electrophysiological and computational approaches we have examined a
series of positive allosteric modulators (PAMs) acting on the human α7 nicotinic acetylcholine …
series of positive allosteric modulators (PAMs) acting on the human α7 nicotinic acetylcholine …
Allosteric agonism of α7 nicotinic acetylcholine receptors: Receptor modulation outside the orthosteric site
A Gulsevin, RL Papke, C Stokes, S Garai… - Molecular …, 2019 - ASPET
Nicotinic acetylcholine receptors (nAChRs) are members of the Cys-loop superfamily of
ligand-gated ion channels. Typically, channel activation follows the binding of agonists to the …
ligand-gated ion channels. Typically, channel activation follows the binding of agonists to the …