NCIt related terms : 2X-121; PARP/Tankyrase Inhibitor 2X-121;
NCIt definition : An orally available small molecule inhibitor of the nuclear enzymes poly (ADP-ribose)
polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration,
E7449 selectively binds to PARP 1 and 2, thereby preventing the repair of damaged
DNA via the base excision repair (BER) pathway. This agent enhances the accumulation
of single and double strand DNA breaks and promotes genomic instability eventually
leading to apoptosis. PARP 1/2 inhibitor E7449 may enhance the cytotoxicity of DNA-damaging
agents and of radiotherapy. PARP catalyzes post-translational ADP-ribosylation of
nuclear proteins that signal and recruit other proteins to repair damaged DNA.;
Semantic type(s)