Trial watch - inhibiting PARP enzymes for anticancer therapy.

摘要: ABSTRACTPoly(ADP-ribose) polymerases (PARPs) are a members of family enzymes that catalyze poly(ADP-ribosyl)ation (PARylation) and/or mono(ADP-ribosyl)ation (MARylation), two post-translational protein modifications involved in crucial cellular processes including (but not limited to) the DNA damage response (DDR). PARP1, most abundant member, is nuclear activated upon sensing distinct types and contributes to their resolution by PARylating multiple DDR players. Recent evidence suggests that, along with DDR, PARP1 mediates series prosurvival proapoptotic aimed at preserving genomic stability. Despite this potential oncosuppressive role, upregulation overactivation or other PARP has been reported variety human neoplasms. Over last few decades, several pharmacologic inhibitors PARP2 have assessed preclinical clinical studies showing potent antineoplastic activity, particula...