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The Bicyclic Form of galacto-Noeurostegine Is a Potent Inhibitor of β-Galactocerebrosidase

  • Agnete Viuff
    Agnete Viuff
    Department of Chemistry, Aarhus University, Langelandsgade 140, 8000 Aarhus C, Denmark
    More by Agnete Viuff
  • Stéphane Salamone
    Stéphane Salamone
    Department of Chemistry, Aarhus University, Langelandsgade 140, 8000 Aarhus C, Denmark
  • Joseph McLoughlin
    Joseph McLoughlin
    Department of Clinical Neuroscience, Cambridge Institute of Medical Research, University of Cambridge, Hills Road, Cambridge CB2 0XY, U.K.
  • Janet E. Deane*
    Janet E. Deane
    Department of Clinical Neuroscience, Cambridge Institute of Medical Research, University of Cambridge, Hills Road, Cambridge CB2 0XY, U.K.
    *Email: [email protected]
  • , and 
  • Henrik H. Jensen*
    Henrik H. Jensen
    Department of Chemistry, Aarhus University, Langelandsgade 140, 8000 Aarhus C, Denmark
    *Email: [email protected]
Cite this: ACS Med. Chem. Lett. 2021, 12, 1, 56–59
Publication Date (Web):December 18, 2020
https://doi.org/10.1021/acsmedchemlett.0c00377
Copyright © 2020 American Chemical Society

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    Abstract

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    Competitive inhibitors of galactocerebrosidase (GALC) could be candidates for pharmacological chaperone therapy of patients with Krabbe disease. The known and selective nortropane-type iminosugar galacto-noeurostegine has been found to competitively inhibit GALC with Ki = 7 μM at pH 4.6, which is 330-fold more potent than the analogous deoxynoeurostegine. It was shown through X-ray protein crystallography that galacto-noeurostegine binds to the active site of GALC in its bicyclic form.

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    The Supporting Information is available free of charge at https://pubs.acs.org/doi/10.1021/acsmedchemlett.0c00377.

    • Detailed experimental description of enzyme inhibition, protein expression/purification/crystallization, X-ray data collection, and differential scanning fluorimetry (PDF)

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    Cited By

    This article is cited by 1 publications.

    1. Camilla Matassini, Francesca Clemente, Francesca Cardona. Carbohydrate‐Based Therapeutics for Lysosomal Storage Disorders. 2023, 245-292. https://doi.org/10.1002/9783527831326.ch9

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