JA2131 is a cell penetrant, potent and selective poly(ADP-ribose) glycohydrolase (PARG) inhibitor that selectively kills cancer cells. JA2131 induces PARP1 hyper-PARylation and sensitizes cancer cells to radiation-induced DNA damage. JA2131 induces replication fork defects.
cell penetrant, potent and selective poly(ADP-ribose) glycohydrolase (PARG) inhibitor
Poly(ADP-ribose)ylation (PARylation) by PAR polymerase 1 (PARP1) and PARylation removal by poly(ADP-ribose) glycohydrolase (PARG) critically regulate DNA damage responses; yet, conflicting reports obscure PARG biology and its impact on cancer cell resistance to PARP1 inhibitors. Here, we found that PARG
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