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Molecular Pharmacology

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Insights into the structure-activity relationship of glycosides as positive allosteric modulators acting on P2X7 receptors

Waraporn Piyasirananda, Andrew Beekman, A. Ganesan, Stefan Bidula and Leanne Stokes
Molecular Pharmacology December 17, 2020, MOLPHARM-AR-2020-000129; DOI: https://doi.org/10.1124/molpharm.120.000129
Waraporn Piyasirananda
1Pharmacy, University of East Anglia, United Kingdom
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Andrew Beekman
1Pharmacy, University of East Anglia, United Kingdom
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A. Ganesan
1Pharmacy, University of East Anglia, United Kingdom
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Stefan Bidula
2University of East Anglia, United Kingdom
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Leanne Stokes
1Pharmacy, University of East Anglia, United Kingdom
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  • ORCID record for Leanne Stokes
  • For correspondence: l.stokes@uea.ac.uk
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  • Data Supplement

    • Supplemental Figures -

      Supplementary Figure 1: Effect of disaccharides stevenleaf and esculentoside A on P2X7.

      Supplementary Figure 2: P2X7 expression in THP-1 monocytes.

    • Supplemental Data -

      Supplemental material: PDB file showing 20(S)-Rg3 docked to a homology model of human P2X7 in the predicted open-state. ATP is also shown within the structure. The model shows the central (most-populated) pose generated using Glide software (Schrodinger suite).

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Molecular Pharmacology: 99 (2)
Molecular Pharmacology
Vol. 99, Issue 2
1 Feb 2021
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P2X7 positive modulator SAR

Waraporn Piyasirananda, Andrew Beekman, A. Ganesan, Stefan Bidula and Leanne Stokes
Molecular Pharmacology December 17, 2020, MOLPHARM-AR-2020-000129; DOI: https://doi.org/10.1124/molpharm.120.000129

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OtherArticle

P2X7 positive modulator SAR

Waraporn Piyasirananda, Andrew Beekman, A. Ganesan, Stefan Bidula and Leanne Stokes
Molecular Pharmacology December 17, 2020, MOLPHARM-AR-2020-000129; DOI: https://doi.org/10.1124/molpharm.120.000129
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