Structures of highly flexible intracellular domain of human α7 nicotinic acetylcholine receptor

V Bondarenko, MM Wells, Q Chen, TS Tillman… - Nature …, 2022 - nature.com
The intracellular domain (ICD) of Cys-loop receptors mediates diverse functions. To date, no
structure of a full-length ICD is available due to challenges stemming from its dynamic …

Structural Elucidation of Ivermectin binding to α7nAChR and the induced channel desensitization

V Bondarenko, Q Chen, K Singewald… - ACS Chemical …, 2023 - ACS Publications
The α7 nicotinic acetylcholine receptor (α7nAChR) mediates signaling in the central nervous
system and cholinergic anti-inflammatory pathways. Ivermectin is a positive allosteric …

Unconventional PDZ Recognition Revealed in α7 nAChR-PICK1 Complexes

V Bondarenko, Q Chen, TS Tillman, Y Xu… - ACS chemical …, 2024 - ACS Publications
PDZ domains are modular domains that conventionally bind to C terminal or internal motifs
of target proteins to control cellular functions through the regulation of protein complex …

Competitive Antagonism of Xylazine on α7 Nicotinic Acetylcholine Receptors and Reversal by Curcuminoids

Q Chen, Y Xu, P Tang - ACS Chemical Neuroscience, 2024 - ACS Publications
Co-use of xylazine with opioids is a major health threat in the United States. However, a
critical knowledge gap exists in the understanding of xylazine-induced pharmacological and …

19F Paramagnetic Relaxation-Based NMR for Quaternary Structural Restraints of Ion Channels

V Bondarenko, MM Wells, Q Chen… - ACS chemical …, 2019 - ACS Publications
Quaternary distance restraints are essential to define the three-dimensional structures of
protein assemblies. These distances often fall within a range of 10–18 Å, which challenges …

Probing function in ligand-gated ion channels without measuring ion transport

NE Godellas, C Grosman - Journal of General Physiology, 2022 - rupress.org
Although the functional properties of ion channels are most accurately assessed using
electrophysiological approaches, a number of experimental situations call for alternative …

The expression of soluble functional α7-nicotinic acetylcholine receptors in E. coli and its high-affinity binding to neonicotinoid pesticides

D Xiang, X Xu, Q Zhou, R Yan, M Chen, Y Guo… - Pesticide biochemistry …, 2020 - Elsevier
Nicotinic acetylcholine receptors (nAChRs) are ligand-gated ion channels mediating fast
cholinergic synaptic transmission in nervous system. In insects, nAChRs are the target sites …

Functional tolerance to cysteine mutations in human α7 nicotinic acetylcholine receptors

TS Tillman, Z Choi, Y Xu, P Tang - ACS chemical neuroscience, 2020 - ACS Publications
The α7 nicotinic acetylcholine receptor (α7 nAChR) is involved in various intracellular
signaling pathways that mediate addiction, chronic pain, and other diseases, but its …

Functional molecular motions in drug design: application to nicotinic acetylcholine receptors

MG Medina - 2022 - theses.hal.science
The study of the conformational changes occurring in a protein structure is essential to
understand its function and how a protein can be modulated. This research project was …

A Comparative Analysis of the Principles Behind α7 Nicotinic Acetylcholine Receptor Function

A Gulsevin - 2017 - search.proquest.com
Silent agonists are α7 nicotinic acetylcholine receptor ligands that do not evoke a response
larger than 10% of the acetylcholine control but put the receptor into a desensitized state (D …