Apoptosis-regulating proteins as targets for drug discovery

Trends Mol Med. 2001 Jul;7(7):314-9. doi: 10.1016/s1471-4914(01)02026-3.


Defects in the regulation of apoptosis (programmed cell death) contribute to many diseases, including pathologies associated with cell loss (e.g. stroke, heart failure, neurodegeneration and AIDS), and disorders characterized by a failure to eliminate harmful cells (e.g. cancer, autoimmunity). Apoptosis is caused by activation of intracellular proteases, known as caspases, which are responsible directly or indirectly for the morphological and biochemical events that characterize the apoptotic cell. Numerous caspase regulators have been discovered, which respond to environmental stimuli and influence the decision of cell death and survival. Knowledge of the molecular details of apoptosis regulation, and the three-dimensional structures of proteins constituting the apoptosis core machinery has revealed new strategies for identifying small-molecule drugs that could one day yield more effective treatments for a wide variety of illnesses.

Publication types

  • Review

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Apoptosis / physiology*
  • Caspases / drug effects
  • Caspases / metabolism
  • Drug Design*
  • Genes, Intracisternal A-Particle / drug effects
  • Humans
  • Mitochondria / metabolism
  • Nucleotides / metabolism
  • Protein Kinases / drug effects
  • Protein Kinases / metabolism
  • Proteins / drug effects*
  • Proteins / metabolism*
  • Proto-Oncogene Proteins c-bcl-2 / drug effects
  • Proto-Oncogene Proteins c-bcl-2 / metabolism


  • Nucleotides
  • Proteins
  • Proto-Oncogene Proteins c-bcl-2
  • Protein Kinases
  • Caspases