ArticleBritish journal of pharmacology2020
In vitro and in silico characterization of the inhibition of Kir4.1 channels by aminoglycoside antibiotics.
Article in British journal of pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 10 citations in OpenAlex.
- Preclinical Insights into the Role of Kir4.1 in Chronic Pain and Depression: Mechanisms and Therapeutic Potential.Biomolecules · 2025Review
- Pharmacological inhibition of Kir4.1 evokes rapid-onset antidepressant responses.Nature chemical biology · 2024Article
- Non-trivial dynamics in a model of glial membrane voltage driven by open potassium pores.Biophysical journal · 2023Article
- Inwardly rectifying potassium channels mediate polymyxin-induced nephrotoxicity.Cellular and molecular life sciences : CMLS · 2022Article
- Emerging Roles of Astrocyte Kir4.1 Channels in the Pathogenesis and Treatment of Brain Diseases.International journal of molecular sciences · 2021Review
- In vitro and in silico characterization of the inhibition of Kir4.1 channels by aminoglycoside antibiotics.British journal of pharmacology · 2020Article
Corrections and comments
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Authors and funding
7 authors at 2 institutions in 3 countries.
Funding
Abstract
background and purposeAminoglycoside antibiotics are positively charged molecules that are known to inhibit several ion channels. In this study, we have shown that aminoglycosides also inhibit the activity of Kir4.1 channels. Aminoglycosides inhibit Kir4.1 channels by a pore-blocking mechanism, plugging the central vestibule of the channel. EXPERIMENTAL APPROACH: Patch-clamp recordings were made in HEK-293 cells transiently expressing Kir4.1 channels to analyse the effects of gentamicin, neomycin and kanamycin. In silico modelling followed by mutagenesis were realized to identify the residues critical for aminoglycosides binding to Kir4.1. KEY
resultsAminoglycoside antibiotics block Kir4.1 channels in a concentration- and voltage-dependent manner, getting access to the protein from the intracellular side of the plasma membrane. Aminoglycosides block Ki4.1 with a rank order of potency as follows: gentamicin ˃ neomycin ˃ kanamycin. The residues T128 and principally E158, facing the central cavity of Kir4.1, are important structural determinants for aminoglycosides binding to the channel, as determined by our in silico modelling and confirmed by mutagenesis experiments. CONCLUSION AND IMPLICATIONS: Kir4.1 channels are also target of aminoglycoside antibiotics, which could affect potassium transport in several tissues.
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