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

Gianluca Papeo1, Barbara Forte, Paolo Orsini

  • 1Department of Medicinal Chemistry, Nerviano Medical Sciences, Viale Pasteur 10, Nerviano (MI), Italy.

Abstract

Insights

Poly(ADP-ribose) polymerase (PARP) inhibitors are increasingly used in cancer therapy. Recent advancements show promising orally available PARP-1 inhibitors for specific cancer types and new therapeutic targets.

Area of Science:

  • Oncology
  • Pharmacology
  • Biochemistry

Background:

  • Poly(ADP-ribose) polymerase (PARP) inhibitors are gaining prominence in cancer treatment.
  • Increased understanding of PARP-1 function and clinical benefits of its inhibition drives this trend.

Purpose of the Study:

  • To provide an update on PARP inhibition in cancer therapy.
  • Review recent scientific and patent literature from 2005-2008.

Main Methods:

  • Comprehensive literature search of scientific databases (SciFinder).
  • Patent literature review (Chemical Abstract/Derwent).

Main Results:

  • Emergence of orally available PARP-1 inhibitor clinical candidates.
  • Identification of specific molecularly defined cancer indications for PARP-1 inhibitors as single agents.

Conclusions:

  • Orally available PARP-1 inhibitors enhance patient compliance and offer new therapeutic options.
  • Other PARP family members, like Tankyrase 1, represent potential future drug targets.
  • Novel PARP inhibitor compounds are being developed, expanding beyond traditional NAD-mimicking structures.

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