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Updated: Jan 23, 2026

Site Directed Spin Labeling and EPR Spectroscopic Studies of Pentameric Ligand-Gated Ion Channels
Published on: July 4, 2016
Ligand Docking to the Acidic Pocket of the Proton-Gated Ion Channel Asic1A
V S Korkosh1,2, D B Tikhonov3,4
1Sechenov Institute of Evolutionary Physiology and Biochemistry, St. Petersburg, Russia.
Abstract:
In this study, we performed the docking of ligands of the ASIC1a ion channel, which exert potentiating or inhibitory effects by stabilizing the open and closed states, respectively. It is shown for the first time that the direction of effect may depend on the three-dimensional structure of the ligand. Potentiators and inhibitors differently interact with the amino acid residues of the so-called "acidic pocket," where the binding of protons takes place. These results open up an opportunity for theoretical design of new pharmaceuticals.
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