Laying a trap to kill cancer cells: PARP inhibitors and their mechanisms of action

Sci Transl Med. 2016 Oct 26;8(362):362ps17. doi: 10.1126/scitranslmed.aaf9246.

Abstract

Poly(ADP-ribose) polymerase (PARP) inhibitors are the first DNA damage response targeted agents approved for cancer therapy. Here, we focus on their molecular mechanism of action by PARP "trapping" and what this means for both clinical monotherapy and combination with chemotherapeutic agents.

MeSH terms

  • Antineoplastic Agents / pharmacology
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / pathology
  • Clinical Trials, Phase I as Topic
  • DNA Damage
  • DNA Repair
  • Enzyme Inhibitors / pharmacology
  • Female
  • Genes, BRCA1
  • Humans
  • Male
  • Maximum Tolerated Dose
  • Mutation
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / pathology
  • Poly(ADP-ribose) Polymerase Inhibitors / pharmacology*
  • Poly(ADP-ribose) Polymerases / chemistry*
  • Prostatic Neoplasms / drug therapy*
  • Prostatic Neoplasms / pathology
  • Translational Research, Biomedical

Substances

  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Poly(ADP-ribose) Polymerase Inhibitors
  • Poly(ADP-ribose) Polymerases