Toward Elucidating the Heat Activation Mechanism of the TRPV1 Channel Gating by Molecular Dynamics Simulation
Sign Up to like & getrecommendations! Published in 2017 at "Biophysical Journal"
DOI: 10.1016/j.bpj.2016.11.638
Abstract: As a key cellular sensor, the TRPV1 cation channel undergoes a gating transition from a closed state to an open state in response to various physical and chemical stimuli including noxious heat. Despite years of… read more here.
Keywords: state; channel; open state; heat activation ... See more keywords
Up-regulation of voltage-gated sodium channels by peptides mimicking S4-S5 linkers reveals a variation of the ligand-receptor mechanism
Sign Up to like & getrecommendations! Published in 2020 at "Scientific Reports"
DOI: 10.1038/s41598-020-62615-6
Abstract: Prokaryotic Na V channels are tetramers and eukaryotic Na V channels consist of a single subunit containing four domains. Each monomer/domain contains six transmembrane segments (S1-S6), S1-S4 being the voltage-sensor domain and S5-S6 the pore… read more here.
Keywords: state; voltage; regulation voltage; gated sodium ... See more keywords
Derivatives of 2-aminobenzimidazole potentiate ASIC open state with slow kinetics of activation and desensitization
Sign Up to like & getrecommendations! Published in 2023 at "Frontiers in Physiology"
DOI: 10.3389/fphys.2023.1018551
Abstract: The pharmacology of acid-sensitive ion channels (ASICs) is diverse, but potent and selective modulators, for instance for ASIC2a, are still lacking. In the present work we studied the effect of five 2-aminobenzimidazole derivatives on native… read more here.
Keywords: open state; state slow; slow kinetics; activation desensitization ... See more keywords
Analysis of Different Binding Modes for Tiagabine within the GAT-1 Transporter
Sign Up to like & getrecommendations! Published in 2022 at "Biomolecules"
DOI: 10.3390/biom12111663
Abstract: The recently obtained cryo-electron microscopy structure (PDB code: 7SK2) of the human γ-aminobutyric acid transporter type 1 (hGAT-1) in complex with the antiepileptic drug, tiagabine, revealed a rather unexpected binding mode for this inhibitor in… read more here.
Keywords: open state; transporter; tiagabine; site ... See more keywords