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Tuning glycosidase inhibition through aglycone interactions: pharmacological chaperones for Fabry disease and GM1 gangliosidosis |
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| Authors: | Aguilar-Moncayo M Takai T Higaki K Mena-Barragán T Hirano Y Yura K Li L Yu Y Ninomiya H García-Moreno M I Ishii S Sakakibara Y Ohno K Nanba E Ortiz Mellet C García Fernández J M Suzuki Y |
| Institution: | Dpto. Química Orgánica, Fac. de Química, Universidad de Sevilla, c/ Professor García González 1, E-41012 Sevilla, Spain. |
| Abstract: | Competitive inhibitors of either α-galactosidase (α-Gal) or β-galactosidase (β-Gal) with high affinity and selectivity have been accessed by exploiting aglycone interactions with conformationally locked sp(2)-iminosugars. Selected compounds were profiled as potent pharmacological chaperones for mutant lysosomal α- and β-Gal associated with Fabry disease and GM(1) gangliosidosis. |
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