The Potential of PARP Inhibitors as Antitumor Drugs and the Perspective of Molecular Design

PARP (poly-ADP ribose polymerase) has received widespread attention in cancer treatment. Research has shown that PARP plays a crucial role in DNA damage repair and has become a popular target for drug design. Based on the mechanism of “synthetic lethality”, multiple PARPis (PARP inhibitors) have been launched for the treatment of BRCA deficient tumors. For example, the approved PARPis have shown significant potential in cancer treatment, particularly in breast cancer and cancers associated with BRCA1/BRCA2 deficiencies. However, the clinical efficacy and safety of PARP inhibitors in different cancers remain issues that cannot be overlooked. The design of PARPis aims to eliminate their resistance and broaden their application scope. Designing selective PARP-1 inhibitors is also a potential strategy. PROTACs (Proteolysis Targeting Chimeras) to degrade PARP have become a potential novel cancer treatment strategy.