PARP1 Inhibitor DSB2455

**Semantic type:** Pharmacologic Substance

**Definition:** An orally bioavailable, central nervous system (CNS) active inhibitor of nuclear enzyme poly(ADP-ribose) polymerase (PARP) 1, with potential antineoplastic activity. Upon oral administration, PARP1 inhibitor DSB2455 selectively binds to and inhibits the activity of PARP1, thereby preventing the repair of damaged DNA via the base excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks and promotes genomic instability eventually leading to apoptosis. PARP1 catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and plays a key role in the repair of single strand DNA (ssDNA) breaks and double-strand breaks (DSBs). DSB2455 is able to cross the blood-brain barrier (BBB).

**Synonyms:** - DSB 2455 - DSB-2455 - DSB2455