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Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems

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Τίτλος: Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems
Συγγραφείς: Kónya, Zoltán, Bécsi, Bálint, Kiss, Andrea, Horváth, Dániel, Hadháziné Raics, Mária, Kövér, Katalin, E., Lontay, Beáta, Erdődi, Ferenc
Πηγή: J Enzyme Inhib Med Chem
Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 500-509 (2019)
Στοιχεία εκδότη: Informa UK Limited, 2019.
Έτος έκδοσης: 2019
Θεματικοί όροι: 0301 basic medicine, Magnetic Resonance Spectroscopy, Synaptosomal-Associated Protein 25, Cell Survival, RM1-950, Calorimetry, tellimagrandin i, Exocytosis, Inhibitory Concentration 50, Mice, Structure-Activity Relationship, 03 medical and health sciences, Protein Phosphatase 1, synaptosomal exocytosis, Animals, Humans, Elméleti orvostudományok, protein phosphatase-2a, Protein Phosphatase 2, Enzyme Inhibitors, Phosphorylation, Muscle, Skeletal, Cerebral Cortex, 0303 health sciences, mahtabin a, protein phosphatase-1, Orvostudományok, Surface Plasmon Resonance, Hydrolyzable Tannins, 3. Good health, Therapeutics. Pharmacology, Research Paper, HeLa Cells, Synaptosomes
Περιγραφή: Several ellagitannins inhibited the activity of protein phosphatase-1 (PP1) and -2 A (PP2A) catalytic subunits (PP1c and PP2Ac) with preferential suppression of PP1c over PP2Ac. The inhibitory potency for PP1c followed the order of tellimagrandin I > mahtabin A > praecoxin B > 1.2-Di-O-galloyl-4.6-(S)-HHDP-β-D-glucopyranose > pedunculagin with IC50 values ranging from 0.20 µM to 2.47 µM. The interaction of PP1c and tellimagrandin I was assessed by NMR saturation transfer difference, surface plasmon resonance, isothermal titration calorimetry, and microscale thermophoresis based binding techniques. Tellimagrandin I suppressed viability and phosphatase activity of HeLa cells, while mahtabin A was without effect. Conversely, mahtabin A increased the phosphorylation level of SNAP-25Thr138 and suppressed exocytosis of cortical synaptosomes, whereas tellimagrandin I was without influence. Our results establish ellagitannins as partially selective inhibitors of PP1 and indicate that these polyphenols may act distinctly in cellular systems depending on their membrane permeability and/or their actions on cell membranes.
Τύπος εγγράφου: Article
Conference object
Other literature type
Περιγραφή αρχείου: application/pdf
Γλώσσα: English
ISSN: 1475-6374
1475-6366
DOI: 10.1080/14756366.2018.1557653
Σύνδεσμος πρόσβασης: https://www.tandfonline.com/doi/pdf/10.1080/14756366.2018.1557653?needAccess=true
https://pubmed.ncbi.nlm.nih.gov/30696301
https://doaj.org/article/1ebea239b38c40f89067b205d3226b25
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6352937/
https://pubmed.ncbi.nlm.nih.gov/30696301/
https://www.tandfonline.com/doi/full/10.1080/14756366.2018.1557653
Rights: CC BY
Αριθμός Καταχώρησης: edsair.doi.dedup.....2c9937d40290307e3fd959f1d1d60e81
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  Data: Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems
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  Data: J Enzyme Inhib Med Chem<br />Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 34, Iss 1, Pp 500-509 (2019)
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  Data: Several ellagitannins inhibited the activity of protein phosphatase-1 (PP1) and -2 A (PP2A) catalytic subunits (PP1c and PP2Ac) with preferential suppression of PP1c over PP2Ac. The inhibitory potency for PP1c followed the order of tellimagrandin I > mahtabin A > praecoxin B > 1.2-Di-O-galloyl-4.6-(S)-HHDP-β-D-glucopyranose > pedunculagin with IC50 values ranging from 0.20 µM to 2.47 µM. The interaction of PP1c and tellimagrandin I was assessed by NMR saturation transfer difference, surface plasmon resonance, isothermal titration calorimetry, and microscale thermophoresis based binding techniques. Tellimagrandin I suppressed viability and phosphatase activity of HeLa cells, while mahtabin A was without effect. Conversely, mahtabin A increased the phosphorylation level of SNAP-25Thr138 and suppressed exocytosis of cortical synaptosomes, whereas tellimagrandin I was without influence. Our results establish ellagitannins as partially selective inhibitors of PP1 and indicate that these polyphenols may act distinctly in cellular systems depending on their membrane permeability and/or their actions on cell membranes.
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  Data: 10.1080/14756366.2018.1557653
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        Value: 10.1080/14756366.2018.1557653
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      – Text: English
    PhysicalDescription:
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        PageCount: 10
        StartPage: 500
    Subjects:
      – SubjectFull: 0301 basic medicine
        Type: general
      – SubjectFull: Magnetic Resonance Spectroscopy
        Type: general
      – SubjectFull: Synaptosomal-Associated Protein 25
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      – SubjectFull: Cell Survival
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      – SubjectFull: tellimagrandin i
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      – SubjectFull: Exocytosis
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      – SubjectFull: Inhibitory Concentration 50
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      – SubjectFull: Structure-Activity Relationship
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      – SubjectFull: Protein Phosphatase 1
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      – SubjectFull: synaptosomal exocytosis
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      – SubjectFull: Animals
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      – SubjectFull: Humans
        Type: general
      – SubjectFull: Elméleti orvostudományok
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      – SubjectFull: protein phosphatase-2a
        Type: general
      – SubjectFull: Protein Phosphatase 2
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      – SubjectFull: Enzyme Inhibitors
        Type: general
      – SubjectFull: Phosphorylation
        Type: general
      – SubjectFull: Muscle, Skeletal
        Type: general
      – SubjectFull: Cerebral Cortex
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      – SubjectFull: 0303 health sciences
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      – SubjectFull: mahtabin a
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      – SubjectFull: Orvostudományok
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      – SubjectFull: Surface Plasmon Resonance
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      – SubjectFull: Hydrolyzable Tannins
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      – SubjectFull: 3. Good health
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      – SubjectFull: Therapeutics. Pharmacology
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      – SubjectFull: Research Paper
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      – SubjectFull: HeLa Cells
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      – SubjectFull: Synaptosomes
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      – TitleFull: Inhibition of protein phosphatase-1 and -2A by ellagitannins: structure-inhibitory potency relationships and influences on cellular systems
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