Poly(ADP-ribose) polymerase family (PARP family)

Poly(ADP-ribose) polymerase family proteins (PARPs) are a group of enzymes that catalyze ADP-ribosylation of target proteins using NAD+ as a substrate, with central roles in DNA repair, chromatin remodeling, and the regulation of cell death. There are at least 17 PARP family members in humans, of which PARP1, PARP2, and tankyrases are the best-characterized. PARPs respond to DNA damage by attaching long, branched chains of poly(ADP-ribose) (PAR) to themselves and other nuclear proteins, facilitating recruitment of DNA repair machinery, and modulating transcription, cell fate decisions, and genome maintenance. PARP inhibition is a clinically validated strategy for cancer therapy, especially for tumors deficient in homologous recombination repair (e.g., BRCA mutant cancers).

Other names

Poly(ADP-ribose) polymerasePARPTankyraseADP-ribosyltransferase family

Inhibition of ADP-ribosylation enzymatic activity\nBlockage of DNA repair pathway, leading to synthetic lethality (especially in cells with BRCA1/2 mutations)\nSensitization of tumor cells to DNA-damaging agents