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  1. Article ; Online: Author Correction: Amantadine inhibits known and novel ion channels encoded by SARS-CoV-2 in vitro.

    Toft-Bertelsen, Trine Lisberg / Jeppesen, Mads Gravers / Tzortzini, Eva / Xue, Kai / Giller, Karin / Becker, Stefan / Mujezinovic, Amer / Bentzen, Bo Hjorth / Andreas, Loren B / Kolocouris, Antonios / Kledal, Thomas Nitschke / Rosenkilde, Mette Marie

    Communications biology

    2021  Volume 4, Issue 1, Page(s) 1402

    Language English
    Publishing date 2021-12-10
    Publishing country England
    Document type Published Erratum
    ISSN 2399-3642
    ISSN (online) 2399-3642
    DOI 10.1038/s42003-021-02940-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Clearance of activity-evoked K

    Toft-Bertelsen, Trine Lisberg / Larsen, Brian Roland / Christensen, Sofie Kjellerup / Khandelia, Himanshu / Waagepetersen, Helle S / MacAulay, Nanna

    Glia

    2020  Volume 69, Issue 1, Page(s) 28–41

    Abstract: The mammalian brain consists of 80% water, which is continuously shifted between different compartments and cellular structures by mechanisms that are, to a large extent, unresolved. Aquaporin 4 (AQP4) is abundantly expressed in glia and ependymal cells ... ...

    Abstract The mammalian brain consists of 80% water, which is continuously shifted between different compartments and cellular structures by mechanisms that are, to a large extent, unresolved. Aquaporin 4 (AQP4) is abundantly expressed in glia and ependymal cells of the mammalian brain and has been proposed to act as a gatekeeper for brain water dynamics, predominantly based on studies utilizing AQP4-deficient mice. However, these mice have a range of secondary effects due to the gene deletion. An efficient and selective AQP4 inhibitor has thus been sorely needed to validate the results obtained in the AQP4
    MeSH term(s) Animals ; Aquaporin 4/genetics ; Aquaporins ; Astrocytes/metabolism ; Edema ; Mice ; Neuroglia/metabolism ; Protein Isoforms ; Rats ; Water/metabolism
    Chemical Substances Aqp4 protein, mouse ; Aqp4 protein, rat ; Aqp9 protein, rat ; Aquaporin 4 ; Aquaporins ; Protein Isoforms ; Water (059QF0KO0R)
    Language English
    Publishing date 2020-06-07
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 639414-0
    ISSN 1098-1136 ; 0894-1491
    ISSN (online) 1098-1136
    ISSN 0894-1491
    DOI 10.1002/glia.23851
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Pannexin 1 activation and inhibition is permeant-selective.

    Nielsen, Brian Skriver / Toft-Bertelsen, Trine Lisberg / Lolansen, Sara Diana / Anderson, Connor L / Nielsen, Morten Schak / Thompson, Roger J / MacAulay, Nanna

    The Journal of physiology

    2020  Volume 598, Issue 2, Page(s) 361–379

    Abstract: Key points: The large-pore channel pannexin 1 (Panx1) is expressed in many cell types and can open upon different, yet not fully established, stimuli. Panx1 permeability is often inferred from channel permeability to fluorescent dyes, but it is ... ...

    Abstract Key points: The large-pore channel pannexin 1 (Panx1) is expressed in many cell types and can open upon different, yet not fully established, stimuli. Panx1 permeability is often inferred from channel permeability to fluorescent dyes, but it is currently unknown whether dye permeability translates to permeability to other molecules. Cell shrinkage and C-terminal cleavage led to a Panx1 open-state with increased permeability to atomic ions (current), but did not alter ethidium uptake. Panx1 inhibitors affected Panx1-mediated ion conduction differently from ethidium permeability, and inhibitor efficiency towards a given molecule therefore cannot be extrapolated to its effects on the permeability of another. We conclude that ethidium permeability does not reflect equal permeation of other molecules and thus is no measure of general Panx1 activity.
    Abstract: Pannexin 1 (Panx1) is a large-pore membrane channel connecting the extracellular milieu with the cell interior. While several activation regimes activate Panx1 in a variety of cell types, the selective permeability of an open Panx1 channel remains unresolved: does a given activation paradigm increase Panx1's permeability towards all permeants equally and does fluorescent dye flux serve as a proxy for biological permeation through an open channel? To explore permeant-selectivity of Panx1 activation and inhibition, we employed Panx1-expressing Xenopus laevis oocytes and HEK293T cells. We report that different mechanisms of activation of Panx1 differentially affected ethidium and atomic ion permeation. Most notably, C-terminal truncation or cell shrinkage elevated Panx1-mediated ion conductance, but had no effect on ethidium permeability. In contrast, extracellular pH changes predominantly affected ethidium permeability but not ionic conductance. High [K
    MeSH term(s) Animals ; Connexins/physiology ; Fluorescent Dyes ; Glutamic Acid ; HEK293 Cells ; Humans ; Ion Channels/physiology ; Lactic Acid ; Nerve Tissue Proteins/physiology ; Oocytes ; Xenopus laevis
    Chemical Substances Connexins ; Fluorescent Dyes ; Ion Channels ; Nerve Tissue Proteins ; PANX1 protein, human ; Lactic Acid (33X04XA5AT) ; Glutamic Acid (3KX376GY7L)
    Language English
    Publishing date 2020-01-06
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 3115-x
    ISSN 1469-7793 ; 0022-3751
    ISSN (online) 1469-7793
    ISSN 0022-3751
    DOI 10.1113/JP278759
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Forskere:Myndighedernes model for genåbningen er fyldt med usikkerheder og fejl

    Toft-Bertelsen, Trine Lisberg / Henningsen, Jo / Alexander, Oliver / Nilsson, Pelle / Juhl, Joakim

    Toft-Bertelsen , T L , Henningsen , J , Alexander , O , Nilsson , P & Juhl , J 2020 , ' Forskere : Myndighedernes model for genåbningen er fyldt med usikkerheder og fejl ' , Videnskab.dk [online] . < https://videnskab.dk/naturvidenskab/forskere-myndighedernes-model-for-genaabningen-er-fyldt-med-usikkerheder-og-fejl >

    2020  

    Abstract: KOMMENTAR: Statens Serum Institut har blandt andet fejlagtigt antaget, at mørketallet er meget højt. Det kan have store konsekvenser og resultere i en ny smittebølge og nedlukning. ...

    Abstract KOMMENTAR: Statens Serum Institut har blandt andet fejlagtigt antaget, at mørketallet er meget højt. Det kan have store konsekvenser og resultere i en ny smittebølge og nedlukning.
    Keywords covid-19 ; covid19
    Language Danish
    Publishing country dk
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  5. Article ; Online: Author Correction

    Trine Lisberg Toft-Bertelsen / Mads Gravers Jeppesen / Eva Tzortzini / Kai Xue / Karin Giller / Stefan Becker / Amer Mujezinovic / Bo Hjorth Bentzen / Loren B. Andreas / Antonios Kolocouris / Thomas Nitschke Kledal / Mette Marie Rosenkilde

    Communications Biology, Vol 4, Iss 1, Pp 1-

    Amantadine inhibits known and novel ion channels encoded by SARS-CoV-2 in vitro

    2021  Volume 2

    Keywords Biology (General) ; QH301-705.5
    Language English
    Publishing date 2021-12-01T00:00:00Z
    Publisher Nature Portfolio
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  6. Article ; Online: Amantadine has potential for the treatment of COVID-19 because it inhibits known and novel ion channels encoded by SARS-CoV-2.

    Toft-Bertelsen, Trine Lisberg / Jeppesen, Mads Gravers / Tzortzini, Eva / Xue, Kai / Giller, Karin / Becker, Stefan / Mujezinovic, Amer / Bentzen, Bo Hjorth / B Andreas, Loren / Kolocouris, Antonios / Kledal, Thomas Nitschke / Rosenkilde, Mette Marie

    Communications biology

    2021  Volume 4, Issue 1, Page(s) 1347

    Abstract: The dire need for COVID-19 treatments has inspired strategies of repurposing approved drugs. Amantadine has been suggested as a candidate, and cellular as well as clinical studies have indicated beneficial effects of this drug. We demonstrate that ... ...

    Abstract The dire need for COVID-19 treatments has inspired strategies of repurposing approved drugs. Amantadine has been suggested as a candidate, and cellular as well as clinical studies have indicated beneficial effects of this drug. We demonstrate that amantadine and hexamethylene-amiloride (HMA), but not rimantadine, block the ion channel activity of Protein E from SARS-CoV-2, a conserved viroporin among coronaviruses. These findings agree with their binding to Protein E as evaluated by solution NMR and molecular dynamics simulations. Moreover, we identify two novel viroporins of SARS-CoV-2; ORF7b and ORF10, by showing ion channel activity in a X. laevis oocyte expression system. Notably, amantadine also blocks the ion channel activity of ORF10, thereby providing two ion channel targets in SARS-CoV-2 for amantadine treatment in COVID-19 patients. A screen of known viroporin inhibitors on Protein E, ORF7b, ORF10 and Protein 3a from SARS-CoV-2 revealed inhibition of Protein E and ORF7b by emodin and xanthene, the latter also blocking Protein 3a. This illustrates a general potential of well-known ion channel blockers against SARS-CoV-2 and specifically a dual molecular basis for the promising effects of amantadine in COVID-19 treatment. We therefore propose amantadine as a novel, cheap, readily available and effective way to treat COVID-19.
    MeSH term(s) Amantadine/pharmacology ; Amiloride/analogs & derivatives ; Amiloride/pharmacology ; Antiviral Agents/pharmacology ; Ion Channels/physiology ; Rimantadine/pharmacology ; SARS-CoV-2/drug effects ; Viral Proteins/physiology
    Chemical Substances Antiviral Agents ; Ion Channels ; Viral Proteins ; Rimantadine (0T2EF4JQTU) ; 5-(N,N-hexamethylene)amiloride (1428-95-1) ; Amiloride (7DZO8EB0Z3) ; Amantadine (BF4C9Z1J53)
    Language English
    Publishing date 2021-12-01
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 2399-3642
    ISSN (online) 2399-3642
    DOI 10.1038/s42003-021-02866-9
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article ; Online: Amantadine has potential for the treatment of COVID-19 because it inhibits known and novel ion channels encoded by SARS-CoV-2

    Trine Lisberg Toft-Bertelsen / Mads Gravers Jeppesen / Eva Tzortzini / Kai Xue / Karin Giller / Stefan Becker / Amer Mujezinovic / Bo Hjorth Bentzen / Loren B. Andreas / Antonios Kolocouris / Thomas Nitschke Kledal / Mette Marie Rosenkilde

    Communications Biology, Vol 4, Iss 1, Pp 1-

    2021  Volume 10

    Abstract: Toft-Bertelsen et al. describe repurposing of anti-influenza drug amantadine and its derivatives ...

    Abstract Toft-Bertelsen et al. describe repurposing of anti-influenza drug amantadine and its derivatives for the treatment of SARS-CoV-2. They show that Amantadine, Emodin and Xanthene show significant blockage of ionchannels formed by SARS-CoV-2 which are crucial for its assembly and pathophysiology.
    Keywords Biology (General) ; QH301-705.5
    Language English
    Publishing date 2021-12-01T00:00:00Z
    Publisher Nature Portfolio
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  8. Article ; Online: Regulation of Ca2+ channels by SNAP-25 via recruitment of syntaxin-1 from plasma membrane clusters.

    Toft-Bertelsen, Trine Lisberg / Ziomkiewicz, Iwona / Houy, Sébastien / Pinheiro, Paulo S / Sørensen, Jakob B

    Molecular biology of the cell

    2016  Volume 27, Issue 21, Page(s) 3329–3341

    Abstract: SNAP-25 regulates ... ...

    Abstract SNAP-25 regulates Ca
    MeSH term(s) Animals ; Calcium/metabolism ; Calcium Channels/metabolism ; Calcium Channels/physiology ; Cell Membrane ; Exocytosis/physiology ; Membrane Proteins/metabolism ; Mice ; Mice, Knockout ; Nerve Tissue Proteins/metabolism ; Patch-Clamp Techniques ; Primary Cell Culture ; Protein Binding ; Synaptosomal-Associated Protein 25/metabolism ; Syntaxin 1/metabolism
    Chemical Substances Calcium Channels ; Membrane Proteins ; Nerve Tissue Proteins ; Snap25 protein, mouse ; Synaptosomal-Associated Protein 25 ; Syntaxin 1 ; Calcium (SY7Q814VUP)
    Language English
    Publishing date 2016--01
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1098979-1
    ISSN 1939-4586 ; 1059-1524
    ISSN (online) 1939-4586
    ISSN 1059-1524
    DOI 10.1091/mbc.E16-03-0184
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: Corrigendum to "Bumepamine, a brain-permeant benzylamine derivative of bumetanide, does not inhibit NKCC1 but is more potent to enhance phenobarbital's antiseizure efficacy" [Neuropharmacology 143 (2018) 186-204].

    Brandt, Claudia / Seja, Patricia / Töllner, Kathrin / Römermann, Kerstin / Hampel, Philip / Kalesse, Markus / Kipper, Andi / Feit, Peter W / Lykke, Kasper / Toft-Bertelsen, Trine Lisberg / Paavilainen, Pauliina / Spoljaric, Inkeri / Puskarjov, Martin / MacAulay, Nanna / Kaila, Kai / Löscher, Wolfgang

    Neuropharmacology

    2018  Volume 143, Page(s) 349–350

    Language English
    Publishing date 2018-10-19
    Publishing country England
    Document type Journal Article ; Published Erratum
    ZDB-ID 218272-5
    ISSN 1873-7064 ; 0028-3908
    ISSN (online) 1873-7064
    ISSN 0028-3908
    DOI 10.1016/j.neuropharm.2018.10.012
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  10. Article ; Online: Bumepamine, a brain-permeant benzylamine derivative of bumetanide, does not inhibit NKCC1 but is more potent to enhance phenobarbital's anti-seizure efficacy.

    Brandt, Claudia / Seja, Patricia / Töllner, Kathrin / Römermann, Kerstin / Hampel, Philip / Kalesse, Markus / Kipper, Andi / Feit, Peter W / Lykke, Kasper / Toft-Bertelsen, Trine Lisberg / Paavilainen, Pauliina / Spoljaric, Inkeri / Puskarjov, Martin / MacAulay, Nanna / Kaila, Kai / Löscher, Wolfgang

    Neuropharmacology

    2018  Volume 143, Page(s) 186–204

    Abstract: Based on the potential role of Na-K-Cl cotransporters (NKCCs) in epileptic seizures, the loop diuretic bumetanide, which blocks the NKCC1 isoforms NKCC1 and NKCC2, has been tested as an adjunct with phenobarbital to suppress seizures. However, because of ...

    Abstract Based on the potential role of Na-K-Cl cotransporters (NKCCs) in epileptic seizures, the loop diuretic bumetanide, which blocks the NKCC1 isoforms NKCC1 and NKCC2, has been tested as an adjunct with phenobarbital to suppress seizures. However, because of its physicochemical properties, bumetanide only poorly penetrates through the blood-brain barrier. Thus, concentrations needed to inhibit NKCC1 in hippocampal and neocortical neurons are not reached when using doses (0.1-0.5 mg/kg) in the range of those approved for use as a diuretic in humans. This prompted us to search for a bumetanide derivative that more easily penetrates into the brain. Here we show that bumepamine, a lipophilic benzylamine derivative of bumetanide, exhibits much higher brain penetration than bumetanide and is more potent than the parent drug to potentiate phenobarbital's anticonvulsant effect in two rodent models of chronic difficult-to-treat epilepsy, amygdala kindling in rats and the pilocarpine model in mice. However, bumepamine suppressed NKCC1-dependent giant depolarizing potentials (GDPs) in neonatal rat hippocampal slices much less effectively than bumetanide and did not inhibit GABA-induced Ca
    MeSH term(s) Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/chemistry ; Anticonvulsants/pharmacokinetics ; Anticonvulsants/pharmacology ; Benzylamines/chemical synthesis ; Benzylamines/chemistry ; Benzylamines/pharmacokinetics ; Benzylamines/pharmacology ; Brain/drug effects ; Brain/metabolism ; Bumetanide/analogs & derivatives ; Bumetanide/chemistry ; Bumetanide/pharmacokinetics ; Bumetanide/pharmacology ; Drug Evaluation, Preclinical ; Drug Synergism ; Epilepsy/drug therapy ; Epilepsy/metabolism ; Female ; Mice ; Oocytes ; Phenobarbital/pharmacokinetics ; Phenobarbital/pharmacology ; Rats, Wistar ; Seizures/drug therapy ; Seizures/metabolism ; Sodium Potassium Chloride Symporter Inhibitors/chemistry ; Sodium Potassium Chloride Symporter Inhibitors/pharmacokinetics ; Sodium Potassium Chloride Symporter Inhibitors/pharmacology ; Solute Carrier Family 12, Member 2/metabolism ; Tissue Culture Techniques ; Xenopus laevis
    Chemical Substances Anticonvulsants ; Benzylamines ; Bumepamine ; Sodium Potassium Chloride Symporter Inhibitors ; Solute Carrier Family 12, Member 2 ; Bumetanide (0Y2S3XUQ5H) ; Phenobarbital (YQE403BP4D)
    Language English
    Publishing date 2018-09-21
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218272-5
    ISSN 1873-7064 ; 0028-3908
    ISSN (online) 1873-7064
    ISSN 0028-3908
    DOI 10.1016/j.neuropharm.2018.09.025
    Database MEDical Literature Analysis and Retrieval System OnLINE

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