The Promise of Selective PARP1 Inhibitors in Cancer Therapy

Poly-(ADP-ribose) polymerase 1 (PARP1) is a critical enzyme involved in the DNA damage response. The therapeutic inhibition of PARP1 has emerged as a promising strategy, particularly in cancers with homologous recombination deficiencies (HRDs). A recent report disclosed the discovery of (S)-G9 as a selective PARP1 inhibitor for clinical development.