NCIt definition : An inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential
chemo- and/or radiosensitizing activity. PARP inhibitor E7016 selectively binds to
PARP and prevents PARP mediated DNA repair of single strand DNA breaks via the base-excision
repair pathway. This enhances the accumulation of DNA strand breaks and promotes genomic
instability and eventually leads to apoptosis. In addition, this agent may enhance
the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy
and radiation therapy. PARP catalyzes post-translational ADP-ribosylation of nuclear
proteins that signal and recruit other proteins to repair damaged DNA and is activated
by single-strand DNA breaks.;
Semantic type(s)