Structure-based mechanism of RyR channel operation by calcium and magnesium ions.

Ryanodine receptors (RyRs) serve for excitation-contraction coupling in skeletal and cardiac muscle cells in a noticeably different way, not fully understood at the molecular level. We addressed the structure of skeletal (RyR1) and cardiac (RyR2) isoforms relevant to gating by Ca2+ and Mg2+ ions (M2...

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Main Authors: Alexandra Zahradníková, Jana Pavelková, Miroslav Sabo, Sefer Baday, Ivan Zahradník
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2025-04-01
Series:PLoS Computational Biology
Online Access:https://doi.org/10.1371/journal.pcbi.1012950
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author Alexandra Zahradníková
Jana Pavelková
Miroslav Sabo
Sefer Baday
Ivan Zahradník
author_facet Alexandra Zahradníková
Jana Pavelková
Miroslav Sabo
Sefer Baday
Ivan Zahradník
author_sort Alexandra Zahradníková
collection DOAJ
description Ryanodine receptors (RyRs) serve for excitation-contraction coupling in skeletal and cardiac muscle cells in a noticeably different way, not fully understood at the molecular level. We addressed the structure of skeletal (RyR1) and cardiac (RyR2) isoforms relevant to gating by Ca2+ and Mg2+ ions (M2+). Bioinformatics analysis of RyR structures ascertained the EF-hand loops as the M2+ binding inhibition site and revealed its allosteric coupling to the channel gate. The intra-monomeric inactivation pathway interacts with the Ca2+-activation pathway in both RyR isoforms, and the inter-monomeric pathway, stronger in RyR1, couples to the gate through the S23*-loop of the neighbor monomer. These structural findings were implemented in the model of RyR operation based on statistical mechanics and the Monod-Wyman-Changeux theorem. The model, which defines closed, open, and inactivated macrostates allosterically coupled to M2+-binding activation and inhibition sites, approximated the open probability data for both RyR1 and RyR2 channels at a broad range of M2+ concentrations. The proposed mechanism of RyR operation provides a new interpretation of the structural and functional data of mammalian RyR channels on common grounds. This may provide a new platform for designing pharmacological interventions in the relevant diseases of skeletal and cardiac muscles. The synthetic approach developed in this work may find general use in deciphering mechanisms of ion channel functions.
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spelling doaj-art-ccfb98dd21f746cfab8e31cb1cf519e22025-08-20T02:22:26ZengPublic Library of Science (PLoS)PLoS Computational Biology1553-734X1553-73582025-04-01214e101295010.1371/journal.pcbi.1012950Structure-based mechanism of RyR channel operation by calcium and magnesium ions.Alexandra ZahradníkováJana PavelkováMiroslav SaboSefer BadayIvan ZahradníkRyanodine receptors (RyRs) serve for excitation-contraction coupling in skeletal and cardiac muscle cells in a noticeably different way, not fully understood at the molecular level. We addressed the structure of skeletal (RyR1) and cardiac (RyR2) isoforms relevant to gating by Ca2+ and Mg2+ ions (M2+). Bioinformatics analysis of RyR structures ascertained the EF-hand loops as the M2+ binding inhibition site and revealed its allosteric coupling to the channel gate. The intra-monomeric inactivation pathway interacts with the Ca2+-activation pathway in both RyR isoforms, and the inter-monomeric pathway, stronger in RyR1, couples to the gate through the S23*-loop of the neighbor monomer. These structural findings were implemented in the model of RyR operation based on statistical mechanics and the Monod-Wyman-Changeux theorem. The model, which defines closed, open, and inactivated macrostates allosterically coupled to M2+-binding activation and inhibition sites, approximated the open probability data for both RyR1 and RyR2 channels at a broad range of M2+ concentrations. The proposed mechanism of RyR operation provides a new interpretation of the structural and functional data of mammalian RyR channels on common grounds. This may provide a new platform for designing pharmacological interventions in the relevant diseases of skeletal and cardiac muscles. The synthetic approach developed in this work may find general use in deciphering mechanisms of ion channel functions.https://doi.org/10.1371/journal.pcbi.1012950
spellingShingle Alexandra Zahradníková
Jana Pavelková
Miroslav Sabo
Sefer Baday
Ivan Zahradník
Structure-based mechanism of RyR channel operation by calcium and magnesium ions.
PLoS Computational Biology
title Structure-based mechanism of RyR channel operation by calcium and magnesium ions.
title_full Structure-based mechanism of RyR channel operation by calcium and magnesium ions.
title_fullStr Structure-based mechanism of RyR channel operation by calcium and magnesium ions.
title_full_unstemmed Structure-based mechanism of RyR channel operation by calcium and magnesium ions.
title_short Structure-based mechanism of RyR channel operation by calcium and magnesium ions.
title_sort structure based mechanism of ryr channel operation by calcium and magnesium ions
url https://doi.org/10.1371/journal.pcbi.1012950
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