Genes and Diseases (Jan 2024)

Mechanism of PARP inhibitor resistance and potential overcoming strategies

  • Xiaoyu Fu,
  • Ping Li,
  • Qi Zhou,
  • Ruyuan He,
  • Guannan Wang,
  • Shiya Zhu,
  • Amir Bagheri,
  • Gary Kupfer,
  • Huadong Pei,
  • Juanjuan Li

Journal volume & issue
Vol. 11, no. 1
pp. 306 – 320

Abstract

Read online

PARP inhibitors (PARPi) are a kind of cancer therapy that targets poly (ADP-ribose) polymerase. PARPi is the first clinically approved drug to exert synthetic lethality by obstructing the DNA single-strand break repair process. Despite the significant therapeutic effect in patients with homologous recombination (HR) repair deficiency, innate and acquired resistance to PARPi is a main challenge in the clinic. In this review, we mainly discussed the underlying mechanisms of PARPi resistance and summarized the promising solutions to overcome PARPi resistance, aiming at extending PARPi application and improving patient outcomes.

Keywords