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Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases
ATP-sensitive potassium channels (K(ATP) channels) play pivotal roles in excitable cells and link cellular metabolism with membrane excitability. The action potential converts electricity into dynamics by ion channel-mediated ion exchange to generate systole, involved in every heartbeat. Activation...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Frontiers Media S.A.
2022
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9274113/ https://www.ncbi.nlm.nih.gov/pubmed/35837280 http://dx.doi.org/10.3389/fphar.2022.868401 |
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author | Wang, Zhicheng Bian, Weikang Yan, Yufeng Zhang, Dai-Min |
author_facet | Wang, Zhicheng Bian, Weikang Yan, Yufeng Zhang, Dai-Min |
author_sort | Wang, Zhicheng |
collection | PubMed |
description | ATP-sensitive potassium channels (K(ATP) channels) play pivotal roles in excitable cells and link cellular metabolism with membrane excitability. The action potential converts electricity into dynamics by ion channel-mediated ion exchange to generate systole, involved in every heartbeat. Activation of the K(ATP) channel repolarizes the membrane potential and decreases early afterdepolarization (EAD)-mediated arrhythmias. K(ATP) channels in cardiomyocytes have less function under physiological conditions but they open during severe and prolonged anoxia due to a reduced ATP/ADP ratio, lessening cellular excitability and thus preventing action potential generation and cell contraction. Small active molecules activate and enhance the opening of the K(ATP) channel, which induces the repolarization of the membrane and decreases the occurrence of malignant arrhythmia. Accumulated evidence indicates that mutation of K(ATP) channels deteriorates the regulatory roles in mutation-related diseases. However, patients with mutations in K(ATP) channels still have no efficient treatment. Hence, in this study, we describe the role of K(ATP) channels and subunits in angiocardiopathy, summarize the mutations of the K(ATP) channels and the functional regulation of small active molecules in K(ATP) channels, elucidate the potential mechanisms of mutant K(ATP) channels and provide insight into clinical therapeutic strategies. |
format | Online Article Text |
id | pubmed-9274113 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-92741132022-07-13 Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases Wang, Zhicheng Bian, Weikang Yan, Yufeng Zhang, Dai-Min Front Pharmacol Pharmacology ATP-sensitive potassium channels (K(ATP) channels) play pivotal roles in excitable cells and link cellular metabolism with membrane excitability. The action potential converts electricity into dynamics by ion channel-mediated ion exchange to generate systole, involved in every heartbeat. Activation of the K(ATP) channel repolarizes the membrane potential and decreases early afterdepolarization (EAD)-mediated arrhythmias. K(ATP) channels in cardiomyocytes have less function under physiological conditions but they open during severe and prolonged anoxia due to a reduced ATP/ADP ratio, lessening cellular excitability and thus preventing action potential generation and cell contraction. Small active molecules activate and enhance the opening of the K(ATP) channel, which induces the repolarization of the membrane and decreases the occurrence of malignant arrhythmia. Accumulated evidence indicates that mutation of K(ATP) channels deteriorates the regulatory roles in mutation-related diseases. However, patients with mutations in K(ATP) channels still have no efficient treatment. Hence, in this study, we describe the role of K(ATP) channels and subunits in angiocardiopathy, summarize the mutations of the K(ATP) channels and the functional regulation of small active molecules in K(ATP) channels, elucidate the potential mechanisms of mutant K(ATP) channels and provide insight into clinical therapeutic strategies. Frontiers Media S.A. 2022-06-28 /pmc/articles/PMC9274113/ /pubmed/35837280 http://dx.doi.org/10.3389/fphar.2022.868401 Text en Copyright © 2022 Wang, Bian, Yan and Zhang. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Pharmacology Wang, Zhicheng Bian, Weikang Yan, Yufeng Zhang, Dai-Min Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases |
title | Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases |
title_full | Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases |
title_fullStr | Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases |
title_full_unstemmed | Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases |
title_short | Functional Regulation of K(ATP) Channels and Mutant Insight Into Clinical Therapeutic Strategies in Cardiovascular Diseases |
title_sort | functional regulation of k(atp) channels and mutant insight into clinical therapeutic strategies in cardiovascular diseases |
topic | Pharmacology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9274113/ https://www.ncbi.nlm.nih.gov/pubmed/35837280 http://dx.doi.org/10.3389/fphar.2022.868401 |
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