Novel activity-based probes for broad-spectrum profiling of retaining β-exoglucosidases in situ and in vivo

Angew Chem Int Ed Engl. 2012 Dec 7;51(50):12529-33. doi: 10.1002/anie.201207771. Epub 2012 Nov 8.

Abstract

A high-end label: Cyclophellitol aziridine-type activity-based probes allow for ultra-sensitive visualization of mammalian β-glucosidases (GBA1, GBA2, GBA3, and LPH) as well as several non-mammalian β-glucosidases (see picture). These probes offer new ways to study β-exoglucosidases, and configurational isomers of the cyclophellitol aziridine core may give activity-based probes targeting other retaining glycosidase families.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aziridines / chemistry
  • Brain / enzymology
  • Cellulases / antagonists & inhibitors
  • Cellulases / genetics
  • Cellulases / metabolism*
  • Cyclohexanols / chemistry
  • Cyclohexanols / metabolism
  • Fluorescent Dyes / chemistry*
  • Hep G2 Cells
  • Humans
  • Isomerism
  • Mice
  • Proteomics
  • Recombinant Proteins / antagonists & inhibitors
  • Recombinant Proteins / biosynthesis
  • Recombinant Proteins / genetics

Substances

  • Aziridines
  • Cyclohexanols
  • Fluorescent Dyes
  • Recombinant Proteins
  • cyclophellitol
  • aziridine
  • Cellulases