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  • An orally bioavailable inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) 1 (PARP1) and 2 (PARP2), with potential antineoplastic activity. Upon oral administration, simmiparib selectively binds to PARP and prevents PARP-mediated DNA repair of breaks in single-stranded DNA via the base excision repair pathway. This induces the accumulation of DNA strand breaks, promotes genomic instability, induces G2/M arrest and leads to apoptosis. PARP is activated by single-strand DNA breaks and catalyzes post-translational ADP-ribosylation of nuclear proteins, which signal and recruit other proteins to repair damaged DNA. Check for \'https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C140553\' active clinical trials using this agent. (\'http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C140553\' NCI Thesaurus)
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