Recent advances on the research of PARP-1 inhibitors

Abstract

Poly(ADP-ribose)polymerase-1 (PARP-1) plays significant roles in the DNA repair process by catalyzing the transfer of ADP-ribose from NAD+ to its receptors. It is a promising anticancer drug target and many PARP-1 inhibitors have been developed and used in the clinical trials. PARP-1 inhibitors could be used not only as chemo/ radiotherapy sensitizers, but also as single agents to selectively kill BRCA deficient cancer cells. In this review, 6 classes of PARP-1 inhibitors with distinct structure scaffold were described in terms of the structure-activity relationships and their binding modes within the catalytic domain of PARP-1.