Photoswitchable inhibitors of human β-glucocerebrosidase

Org Biomol Chem. 2022 Feb 23;20(8):1637-1641. doi: 10.1039/d1ob02159a.

Abstract

Light-switchable inhibitors of the enzyme β-glucocerebrosidase (GCase) have been developed by anchoring a specific azasugar to a dihydroazulene or an azobenzene responsive moiety. Their inhibitory effect towards human GCase, before and after irradiation are reported, and the effect on thermal denaturation of recombinant GCase and cytotoxicity were studied on selected candidates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Azo Compounds / chemical synthesis
  • Azo Compounds / chemistry
  • Azo Compounds / pharmacology*
  • Azulenes / chemical synthesis
  • Azulenes / chemistry
  • Azulenes / pharmacology*
  • Cell Line
  • Cell Survival / drug effects
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Glucosylceramidase / antagonists & inhibitors*
  • Glucosylceramidase / metabolism
  • Humans
  • Light
  • Molecular Structure
  • Photochemical Processes

Substances

  • Azo Compounds
  • Azulenes
  • Enzyme Inhibitors
  • dihydroazulene
  • GBA protein, human
  • Glucosylceramidase
  • azobenzene