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lüll Targeting poly(ADP-ribose) polymerase activity for cancer therapy Megnin-Chanet F; Bollet MA; Hall JCell Mol Life Sci 2010[Nov]; 67 (21): 3649-62Poly(ADP-ribosyl)ation is a ubiquitous protein modification found in mammalian cells that modulates many cellular responses, including DNA repair. The poly(ADP-ribose) polymerase (PARP) family catalyze the formation and addition onto proteins of negatively charged ADP-ribose polymers synthesized from NAD(+). The absence of PARP-1 and PARP-2, both of which are activated by DNA damage, results in hypersensitivity to ionizing radiation and alkylating agents. PARP inhibitors that compete with NAD(+) at the enzyme's activity site are effective chemo- and radiopotentiation agents and, in BRCA-deficient tumors, can be used as single-agent therapies acting through the principle of synthetic lethality. Through extensive drug-development programs, third-generation inhibitors have now entered clinical trials and are showing great promise. However, both PARP-1 and PARP-2 are not only involved in DNA repair but also in transcription regulation, chromatin modification, and cellular homeostasis. The impact on these processes of PARP inhibition on long-term therapeutic responses needs to be investigated.|*Poly(ADP-ribose) Polymerase Inhibitors[MESH]|Animals[MESH]|Antineoplastic Agents/pharmacology/*therapeutic use[MESH]|Enzyme Inhibitors/pharmacology/*therapeutic use[MESH]|Humans[MESH]|Neoplasms/*drug therapy/*enzymology[MESH]|Poly(ADP-ribose) Polymerases/*metabolism[MESH] |