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In response to DNA damage, cells can pause the cell cycle to assess and repair the breaks. However, the cell must check the DNA at certain critical stages during the cell cycle. If the cell cycle pauses before DNA replication, the cells will contain twice the amount of DNA. On the other hand, if cells arrest after DNA replication but before mitosis, they will contain four times the normal amount of DNA. With a host of specialized proteins at their disposal,cells must use the right protein at...
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PARP inhibition: PARP1 and beyond.

Michèle Rouleau1, Anand Patel, Michael J Hendzel

  • 1Laval University Medical Research Center, Laval University, Québec, Canada.

Nature Reviews. Cancer
|March 5, 2010
PubMed
Summary

Poly(ADP-ribose) polymerases (PARPs) show promise as cancer drug targets. This review covers PARP enzyme structures and functions, guiding the development of novel PARP inhibitors for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Poly(ADP-ribose) polymerases (PARPs) are emerging as significant targets in cancer chemotherapy.
  • Understanding the diverse roles of PARP enzymes is crucial for therapeutic development.

Purpose of the Study:

  • To review the known structures and functions of the PARP enzyme family.
  • To identify key questions for the rational design of PARP inhibitors as anticancer agents.

Main Methods:

  • Literature review of existing research on PARP enzymes.
  • Analysis of structural and functional data of PARP family members.

Main Results:

  • Comprehensive overview of PARP enzyme structures and biochemical activities.

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  • Identification of critical knowledge gaps in PARP biology relevant to drug development.

    • Conclusions:

    • PARP inhibitors represent a promising avenue for cancer treatment.
    • Further research is needed to address specific questions to optimize PARP inhibitor therapies.