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ID: ALA4673386

Journal: ACS Med Chem Lett

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

Authors: Viuff A,Salamone S,McLoughlin J,Deane JE,Jensen HH

Abstract: 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 K = 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.

CiteXplore: 33488964

DOI: 10.1021/acsmedchemlett.0c00377