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

Authors

Ashmus, Roger A. , Wang, Yang , GONZALEZ CUESTA, MANUEL, King, Dustin T. , Tiet, Ben , Gilormini, Pierre-Andre , Garcia Fernandez, Jose M. , Ortiz Mellet, Carmen , Britton, Robert , Vocadlo, David J.

External publication

No

Means

Org. Biomol. Chem.

Scope

Article

Nature

Científica

JCR Quartile

1

SJR Quartile

1

JCR Impact

3.89

SJR Impact

0.832

Publication date

07/10/2021

ISI

000693679500001

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 (similar to 100-fold) can act in Fabry patient cells to drive reductions in levels of the disease-relevant glycolipid Gb3.

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