Development of an activity-based probe and in silico design reveal highly selective inhibitors for diacylglycerol lipase-α in brain

Angew Chem Int Ed Engl. 2013 Nov 11;52(46):12081-5. doi: 10.1002/anie.201306295. Epub 2013 Oct 31.
No abstract available

Keywords: activity-based probe; drug discovery; endocannabinoid; hydrolases; proteomics.

MeSH terms

  • Animals
  • Arachidonic Acids / metabolism
  • Binding Sites
  • Brain / enzymology*
  • Brain / metabolism
  • Cell Membrane / metabolism
  • Endocannabinoids / metabolism
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / metabolism
  • Glycerides / metabolism
  • HEK293 Cells
  • Humans
  • Lipoprotein Lipase / antagonists & inhibitors
  • Lipoprotein Lipase / genetics
  • Lipoprotein Lipase / metabolism*
  • Mice
  • Protein Binding
  • Protein Structure, Tertiary
  • Proteome
  • Structure-Activity Relationship

Substances

  • Arachidonic Acids
  • Endocannabinoids
  • Enzyme Inhibitors
  • Glycerides
  • Proteome
  • glyceryl 2-arachidonate
  • Lipoprotein Lipase