NCIt definition : A small-molecule prodrug of CEP-8983, a novel 4-methoxy-carbazole inhibitor of the
nuclear enzymes poly(ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic
activity. Upon administration and conversion from CEP-9722, CEP-8983 selectively binds
to PARP 1 and 2, preventing repair of damaged DNA via base excision repair (BER).
This agent enhances the accumulation of DNA strand breaks and promotes genomic instability
and apoptosis. CEP-8983 may potentiate the cytotoxicity of DNA-damaging agents and
reverse tumor cell chemo- and radioresistance. PARP catalyzes post-translational ADP-ribosylation
of nuclear proteins that signal and recruit other proteins to repair damaged DNA and
can be activated by single strand breaks in DNA.;