Small Molecule Active Site Directed Tools for Studying Human Caspases

Chem Rev. 2015 Nov 25;115(22):12546-629. doi: 10.1021/acs.chemrev.5b00434. Epub 2015 Nov 9.


Caspases are proteases of clan CD and were described for the first time more than two decades ago. They play critical roles in the control of regulated cell death pathways including apoptosis and inflammation. Due to their involvement in the development of various diseases like cancer, neurodegenerative diseases, or autoimmune disorders, caspases have been intensively investigated as potential drug targets, both in academic and industrial laboratories. This review presents a thorough, deep, and systematic assessment of all technologies developed over the years for the investigation of caspase activity and specificity using substrates and inhibitors, as well as activity based probes, which in recent years have attracted considerable interest due to their usefulness in the investigation of biological functions of this family of enzymes.

Publication types

  • Review

MeSH terms

  • Caspase Inhibitors / chemistry
  • Caspase Inhibitors / pharmacology*
  • Caspases / chemistry
  • Caspases / metabolism*
  • Catalytic Domain / drug effects
  • Humans
  • Molecular Structure
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*
  • Structure-Activity Relationship


  • Caspase Inhibitors
  • Small Molecule Libraries
  • Caspases