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
i = 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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