parp-1 inhibitor

PARP-1 inhibitors are a class of pharmacological agents designed to selectively block the activity of poly (ADP-ribose) polymerase 1 (PARP-1), an enzyme critical for the repair of single-strand DNA breaks via the base excision repair (BER) pathway. By inhibiting PARP-1, these drugs cause the accumulation of DNA damage, which in cells with deficient homologous recombination repair (HRR) mechanisms—such as those with BRCA1 or BRCA2 mutations—leads to the formation of double-strand breaks and subsequent synthetic lethality. While many first-generation PARP inhibitors target both PARP-1 and PARP-2, newer generation agents are being developed with high selectivity for PARP-1 to potentially reduce hematological toxicities associated with PARP-2 inhibition. Beyond their established role in HR-deficient cancers like ovarian and breast cancer, PARP-1 inhibitors are being investigated as radio-sensitizers in various solid tumors, including renal cell carcinoma, where they may overcome radio-resistance by preventing the repair of radiation-induced DNA damage.

Other names

parp-1 inhibitorparp1 inhibitorparp 1 inhibitorpoly (ADP-ribose) polymerase-1 inhibitor