Poly(ADP-ribose) polymerase inhibition in cancer therapy: Are we close to maturity?

Gianluca Papeo, Barbara Forte, Paolo Orsini, Claudia Perrera, Helena Posteri, Alessandra Scolaro, Alessia Montagnoli (Lead / Corresponding author)

Research output: Contribution to journalReview articlepeer-review

38 Citations (Scopus)


Background: During the last few years an increasing number of poly(ADP-ribose) polymerase (PARP) inhibitors have been appearing in the context of cancer therapy. This is mainly due to a better knowledge of the best-characterized member of the PARP family of enzymes, PARP-1, further reinforced by the recognition of the clinical benefits arising from its inhibition. Objective/method: The aim of this review is to give the reader an update on PARP inhibition in cancer therapy, by covering both the scientific (SciFinder® search) and the patent literature (Chemical Abstract®/ Derwent® search) published recently (2005 - 2008). Conclusions: More patient-compliant orally available PARP-1 inhibitor clinical candidates, along with their possible use as single agents in specific, molecularly defined cancer indications, increase the expectations for this therapeutic approach. The growing understanding of the biological role of other PARPs, such as Tankyrase 1, may be of interest as new potential targets. Besides the classical NAD-mimicking pharmacophore, additional compounds, which either do not resemble nicotinamide or exploit different binding sites, are emerging.

Original languageEnglish
Pages (from-to)1377-1400
Number of pages24
JournalExpert Opinion on Therapeutic Patents
Issue number10
Early online date10 Sept 2009
Publication statusPublished - Oct 2009


  • BRCA
  • Cancer therapy
  • PARP inhibitors
  • Poly(ADP-ribose) polymerase
  • Tankyrase

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery


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