Potent and specific inhibition of glycosidases by small artificial binding proteins (affitins).

ABSTRACT: Glycosidases are associated with various human diseases. The development of efficient and specific inhibitors may provide powerful tools to modulate their activity. However, achieving high selectivity is a major challenge given that glycosidases with different functions can have similar enzymatic mechanisms and active-site architectures. As an alternative approach to small-chemical compounds, proteinaceous inhibitors might provide a better specificity by involving a larger surface area of interaction. We report here the design and characterization of proteinaceous inhibitors that specifically target endoglycosidases representative of the two major mechanistic classes; retaining and inverting glycosidases. These inhibitors consist of artificial affinity proteins, Affitins, selected against

SUBMITTER: Correa A 

PROVIDER: S-EPMC4019568 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature