Definition

An orally bioavailable, small molecule inhibitor of poly (ADP-Ribose) (PAR) glycohydrolase (PARG), with potential antineoplastic activity. Upon oral administration, PARG inhibitor ETX-19477 targets, reversibly binds to and inhibits the activity of PARG, thereby inhibiting the hydrolysis of PAR chains by PARG. This attenuates DNA repair and induces mitotic arrest, ultimately leading to apoptosis of cancer cells. PARG, the only enzyme responsible for hydrolyzing PAR chains produced by poly (ADP-ribose) polymerase (PARP) 1, plays a key role in the resolution of PARP 1/2-dependent DNA damage repair.