Definition

An orally bioavailable, small molecule inhibitor of the nuclear enzymes poly (ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon oral administration, PARP 1/2 inhibitor RP12146 selectively binds to and inhibits PARP-1 and -2, thereby preventing PARP-1 and -2-mediated DNA repair. This promotes genetic instability and enhances the accumulation of single and double strand DNA breaks, ultimately leading to apoptosis. The PARP family of proteins catalyzes post-translational ADP-ribosylation of nuclear proteins and is activated by single-strand DNA (ssDNA) breaks.