Polymeric iminosugars improve the activity of carbohydrate-processing enzymes.
Bioconjug Chem
; 26(4): 766-72, 2015 Apr 15.
Article
em En
| MEDLINE
| ID: mdl-25741759
ABSTRACT
Multivalent iminosugars have recently emerged as powerful tools to inhibit the activities of specific glycosidases. In this work, biocompatible dextrans were coated with iminosugars to form linear and ramified polymers with unprecedently high valencies (from 20 to 900) to probe the evolution of the multivalent inhibition as a function of ligand valency. This study led to the discovery that polyvalent iminosugars can also significantly enhance, not only inhibit, the enzymatic activity of specific glycoside-hydrolase, as observed on two galactosidases, a fucosidase, and a bacterial mannoside phosphorylase for which an impressive 70-fold activation was even reached. The concept of glycosidase activation is largely unexplored, with a unique recent example of small-molecules activators of a bacterial O-GlcNAc hydrolase. The possibility of using these polymers as "artificial enzyme effectors" may therefore open up new perspectives in therapeutics and biocatalysis.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Dextranos
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Materiais Revestidos Biocompatíveis
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Imino Açúcares
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Glicosídeo Hidrolases
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article