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Keywords:

  • ClpP;
  • enzyme inhibitors;
  • lactones;
  • molecular docking;
  • structure–activity relationship
Thumbnail image of graphical abstract

Catch me if you can: The ClpP protease mediates protein homeostasis and can be efficiently inhibited by β-lactones. A combination of molecular docking, mutagenesis, activity-based protein profiling, and kinetics studies now reveals the mechanism of ClpP inhibition. A hydrophobic pocket next to the active site allows binding of long aliphatic and aromatic residues. The preferred stereoisomer binds into the oxyanion hole.