Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).

@article{Steffen2011DiscoveryAS,
  title={Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).},
  author={Jamin D. Steffen and Donna L. Coyle and Komath Damodaran and Paul Beroza and Myron K. Jacobson},
  journal={Journal of medicinal chemistry},
  year={2011},
  volume={54 15},
  pages={5403-13}
}
The metabolism of poly(ADP-ribose) (PAR) in response to DNA strand breaks, which involves the concerted activities of poly(ADP-ribose) polymerases (PARPs) and poly(ADP-ribose) glycohydrolase (PARG), modulates cell recovery or cell death depending upon the level of DNA damage. While PARP inhibitors show high promise in clinical trials because of their low toxicity and selectivity for BRCA related cancers, evaluation of the therapeutic potential of PARG is limited by the lack of well-validated… CONTINUE READING