scholarly journals Insect RDL Receptor Models for Virtual Screening: Impact of the Template Conformational State in Pentameric Ligand-Gated Ion Channels

ACS Omega ◽  
2022 ◽  
Author(s):  
Iván Felsztyna ◽  
Marcos A. Villarreal ◽  
Daniel A. García ◽  
Virginia Miguel
Keyword(s):  
Ion Channels ◽  
Virtual Screening ◽  
Conformational State ◽  
Receptor Models ◽  
Gated Ion Channels ◽  
Ligand Gated Ion Channels

scholarly journals Functional Validation of Virtual Screening for Novel Agents with General Anesthetic Action at Ligand-Gated Ion Channels

2013 ◽  
Vol 84 (5) ◽  
pp. 670-678 ◽  
Author(s):  
Stephanie A. Heusser ◽  
Rebecca J. Howard ◽  
Cecilia M. Borghese ◽  
Madeline A. Cullins ◽  
Torben Broemstrup ◽  
...  
Keyword(s):  
Ion Channels ◽  
Virtual Screening ◽  
Novel Agents ◽  
General Anesthetic ◽  
Functional Validation ◽  
Anesthetic Action ◽  
Gated Ion Channels ◽  
Ligand Gated Ion Channels

An Electrophysiological Study Of The Effects Of Propofol On Native Neuronal Ligand-Gated Ion Channels

2001 ◽  
Vol 28 (5-6) ◽  
pp. 451-458 ◽  
Author(s):  
Debra Patten ◽  
Graham R Foxon ◽  
Keith F Martin ◽  
Robert F Halliwell
Keyword(s):  
Ion Channels ◽  
Electrophysiological Study ◽  
Gated Ion Channels ◽  
Ligand Gated Ion Channels

Physiology and biophysics of plant ligand-gated ion channels

Plant Biology ◽  
2010 ◽  
Vol 12 ◽  
pp. 80-93 ◽  
Author(s):  
P. Dietrich ◽  
U. Anschütz ◽  
A. Kugler ◽  
D. Becker
Keyword(s):  
Ion Channels ◽  
Gated Ion Channels ◽  
Ligand Gated Ion Channels

scholarly journals Molecular Simulations of Hydrophobic Gating of Pentameric Ligand Gated Ion Channels: Insights into Water and Ions

2021 ◽  
Vol 125 (4) ◽  
pp. 981-994
Author(s):  
Shanlin Rao ◽  
Gianni Klesse ◽  
Charlotte I. Lynch ◽  
Stephen J. Tucker ◽  
Mark S. P. Sansom
Keyword(s):  
Ion Channels ◽  
Molecular Simulations ◽  
Gated Ion Channels ◽  
Ligand Gated Ion Channels

Ligand-gated ion channels as targets of neuroactive insecticides

2021 ◽  
Author(s):  
Makoto Ihara
Keyword(s):  
Ion Channels ◽  
Molecular Mechanisms ◽  
Functional Expression ◽  
X Ray ◽  
Acetylcholine Binding Protein ◽  
Site Selectivity ◽  
Future Drug ◽  
Cl Channels ◽  
Gated Ion Channels ◽  
Ligand Gated Ion Channels

Abstract The Cys-loop superfamily of ligand-gated ion channels (Cys-loop receptors) is one of the most ubiquitous ion channel families in vertebrates and invertebrates. Despite their ubiquity, they are targeted by several classes of pesticides, including neonicotinoids, phenylpyrazols, and macrolides such as ivermectins. The current commercialized compounds have high target site selectivity, which contributes to the safety of insecticide use. Structural analyses have accelerated progress in this field; notably, the X-ray crystal structures of acetylcholine binding protein and glutamate-gated Cl channels revealed the details of the molecular interactions between insecticides and their targets. Recently, the functional expression of the insect nicotinic acetylcholine receptor (nAChR) has been described, and detailed evaluations using the insect nAChR have emerged. This review discusses the basic concepts and the current insights into the molecular mechanisms of neuroactive insecticides targeting the ligand-gated ion channels, particularly Cys-loop receptors, and presents insights into target-based selectivity, resistance, and future drug design.

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