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Ashmus RA, Wang Y, González-Cuesta M, et al. Rational design of cell active C2-modified DGJ analogues for the inhibition of human α-galactosidase A (GALA). Org Biomol Chem. 2021;19(37):8057-8062doi: 10.1039/d1ob01526e.
Ashmus, R. A., Wang, Y., González-Cuesta, M., King, D. T., Tiet, B., Gilormini, P. A., García Fernández, J. M., Ortiz Mellet, C., Britton, R., & Vocadlo, D. J. (2021). Rational design of cell active C2-modified DGJ analogues for the inhibition of human α-galactosidase A (GALA). Organic & biomolecular chemistry, 19(37), 8057-8062. https://doi.org/10.1039/d1ob01526e
Ashmus, Roger A, et al. "Rational design of cell active C2-modified DGJ analogues for the inhibition of human α-galactosidase A (GALA)." Organic & biomolecular chemistry vol. 19,37 (2021): 8057-8062. doi: https://doi.org/10.1039/d1ob01526e
Ashmus RA, Wang Y, González-Cuesta M, King DT, Tiet B, Gilormini PA, García Fernández JM, Ortiz Mellet C, Britton R, Vocadlo DJ. Rational design of cell active C2-modified DGJ analogues for the inhibition of human α-galactosidase A (GALA). Org Biomol Chem. 2021 Sep 29;19(37):8057-8062. doi: 10.1039/d1ob01526e. PMID: 34494637.
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Org Biomol Chem. 2021 Sep 29;19(37):8057-8062. doi: 10.1039/d1ob01526e.

Rational design of cell active C2-modified DGJ analogues for the inhibition of human α-galactosidase A (GALA).

Organic & biomolecular chemistry

Roger A Ashmus, Yang Wang, Manuel González-Cuesta, Dustin T King, Ben Tiet, Pierre-André Gilormini, José M García Fernández, Carmen Ortiz Mellet, Robert Britton, David J Vocadlo

Affiliations

  1. Department of Chemistry and Simon Fraser University, Burnaby, British Columbia, Canada. [email protected].
  2. Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, Sevilla 41012, Spain.
  3. Department of Molecular Biology and Biochemistry Simon Fraser University, Burnaby, British Columbia, Canada.
  4. Instituto de Investigaciones Químicas (IIQ), CSIC-Universidad de Sevilla, Sevilla 41092, Spain.

PMID: 34494637 DOI: 10.1039/d1ob01526e

Abstract

We report the rational design and synthesis of C2-modified DGJ analogues to improve the selective inhibition of human GALA over other glycosidases. We prepare these analogues using a concise route from non-carbohydrate materials and demonstrate the most selective inhibitor 7c (∼100-fold) can act in Fabry patient cells to drive reductions in levels of the disease-relevant glycolipid Gb3.

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