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Probing the Inhibitor versus Chaperone Properties of sp2-Iminosugars towards Human -Glucocerebrosidase: A Picomolar Chaperone for Gaucher Disease

Opened Access Probing the Inhibitor versus Chaperone Properties of sp2-Iminosugars towards Human -Glucocerebrosidase: A Picomolar Chaperone for Gaucher Disease

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Autor: Mena-Barragán, Teresa
García-Moreno, M. Isabel
Sevšek, Alen
Okazaki, Tetsuya
Nanba, Eiji
Higaki, Katsumi
Martin, Nathaniel I.
Pieteres, Roland J.
García-Fernández, José Manuel
Ortíz Mellet, María del Carmen
Departamento: Universidad de Sevilla. Departamento de Química Orgánica
Fecha: 2018
Publicado en: Molecules, 23 (4), 927-944.
Tipo de documento: Artículo
Resumen: A series of sp2-iminosugar glycomimetics differing in the reducing or nonreducing character, the configurational pattern (d-gluco or l-ido), the architecture of the glycone skeleton, and the nature of the nonglycone substituent has been synthesized and assayed for their inhibition properties towards commercial glycosidases. On the basis of their affinity and selectivity towards GH1 β-glucosidases, reducing and nonreducing bicyclic derivatives having a hydroxylation profile of structural complementarity with d-glucose and incorporating an N′-octyl-isourea or -isothiourea segment were selected for further evaluation of their inhibitory/chaperoning potential against human glucocerebrosidase (GCase). The 1-deoxynojirimycin (DNJ)-related nonreducing conjugates behaved as stronger GCase inhibitors than the reducing counterparts and exhibited potent chaperoning capabilities in Gaucher fibroblasts hosting the neuronopathic G188S/G183W mutation, the isothiourea derivative being indeed one of t...
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Cita: Mena-Barragán, T., García-Moreno, M.I., Sevšek, A., Okazaki, T., Nanba, E., Higaki, K.,...,Ortíz-Mellet, C. (2018). Probing the Inhibitor versus Chaperone Properties of sp2-Iminosugars towards Human -Glucocerebrosidase: A Picomolar Chaperone for Gaucher Disease. Molecules, 23 (4), 927-944.
Tamaño: 2.221Mb
Formato: PDF

URI: https://hdl.handle.net/11441/74515

DOI: 10.3390/molecules23040927

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