Gating kinetics and pharmacological properties of small-conductance Ca

Potassium Channels Small-Conductance Calcium-Activated Potassium Channels / metabolism Apamin / pharmacology Acetamides Kinetics Calcium / metabolism

Journal

Biophysical journal
ISSN: 1542-0086
Titre abrégé: Biophys J
Pays: United States
ID NLM: 0370626

Informations de publication

Date de publication:
04 04 2023
Historique:
received: 20 07 2022
revised: 20 11 2022
accepted: 06 02 2023
pmc-release: 04 04 2024
medline: 7 4 2023
pubmed: 11 2 2023
entrez: 10 2 2023
Statut: ppublish

Résumé

Small-conductance (SK) calcium-activated potassium channels are a promising treatment target in atrial fibrillation. However, the functional properties that differentiate SK inhibitors remain poorly understood. The objective of this study was to determine how two unrelated SK channel inhibitors, apamin and AP14145, impact SK channel function in excised inside-out single-channel recordings. Surprisingly, both apamin and AP14145 exert much of their inhibition by inducing a class of very-long-lived channel closures (apamin: τ

Identifiants

DOI: 10.1016/j.bpj.2023.02.004 PMID: 36760125 PMC: PMC10111258
pubmed: 36760125
pii: S0006-3495(23)00096-6
doi: 10.1016/j.bpj.2023.02.004
pmc: PMC10111258
pii:
doi:

Substances chimiques

Potassium Channels 0
AP14145 0
Small-Conductance Calcium-Activated Potassium Channels 0
Apamin 24345-16-2
Acetamides 0
Calcium SY7Q814VUP

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

1143-1157

Informations de copyright

Copyright © 2023 Biophysical Society. Published by Elsevier Inc. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of interests B.H.B. is an employee of, and has financial interest in, Acesion Pharma ApS, a developer of SK targeting compounds including AP14145.

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Auteurs

Ilsbeth G M van Herck (IGM)

Computational Physiology Department, Simula Research Laboratory, Oslo, Norway; Institute of Informatics, University of Oslo, Oslo, Norway.

Vincent Seutin (V)

Neurophysiology Unit, GIGA Neurosciences, University of Liège, Liège, Belgium.

Bo H Bentzen (BH)

Acesion Pharma, Copenhagen, Denmark; Biomedical Institute, University of Copenhagen, Copenhagen, Denmark.

Neil V Marrion (NV)

School of Physiology, Pharmacology and Neuroscience, University of Bristol, Bristol, UK.

Andrew G Edwards (AG)

Computational Physiology Department, Simula Research Laboratory, Oslo, Norway; Department of Pharmacology, University of California, Davis, California. Electronic address: andy@simula.no.

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Canaux ioniques › Canaux potassiques › Gating kinetics and pharmacological properties...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines membranaires › Protéines de transport membranaire › Canaux ioniques › Canaux potassiques › Canaux potassiques calcium-dépendants › Canaux potassiques calcium-dépendants de petite conductance › Gating kinetics and pharmacological properties...
questionsmedicales.fr › Facteurs biologiques › Toxines biologiques › Venins › Venins d'arthropode › Venins d'abeille › Apamine › Gating kinetics and pharmacological properties...
questionsmedicales.fr › Composés chimiques organiques › Acides carboxyliques › Acides acycliques › Acétamides › Gating kinetics and pharmacological properties...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Gating kinetics and pharmacological properties...
questionsmedicales.fr › Facteurs biologiques › Facteurs de la coagulation sanguine › Calcium › Gating kinetics and pharmacological properties...