Identification of acyl protein thioesterases 1 and 2 as the cellular targets of the Ras-signaling modulators palmostatin B and M

Angew Chem Int Ed Engl. 2011 Oct 10;50(42):9838-42. doi: 10.1002/anie.201102967. Epub 2011 Sep 9.

Abstract

Finding the target: activity-based proteomic profiling probes based on the depalmitoylation inhibitors palmostatin B and M have been synthesized and were found to target acyl protein thioesterase 1 (APT1) and 2 (APT2) in cells.

MeSH terms

  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Fatty Acid Synthases / antagonists & inhibitors*
  • HeLa Cells
  • Humans
  • Molecular Structure
  • Palmitoyl-CoA Hydrolase / antagonists & inhibitors*
  • Propiolactone / analogs & derivatives*
  • Propiolactone / chemistry
  • Propiolactone / pharmacology
  • Proteome
  • Signal Transduction / drug effects*
  • Structure-Activity Relationship
  • Sulfones / chemistry
  • Sulfones / pharmacology*
  • Thiolester Hydrolases / antagonists & inhibitors*
  • ras Proteins / metabolism*

Substances

  • Enzyme Inhibitors
  • Proteome
  • Sulfones
  • palmostatin B
  • palmostatin M
  • Propiolactone
  • Fatty Acid Synthases
  • Thiolester Hydrolases
  • thioesterase II
  • Palmitoyl-CoA Hydrolase
  • ras Proteins