Olaparib mechanism of action

Olaparib is a selective and potent inhibitor of the poly(ADP-ribose) polymerase (PARP) enzymes PARP1 and PARP2. PARPinhibitors represent a new class of anticancer therapies that work by exploiting defects in DNA repair in cancer cells with BRCA mutations and inducing cell death. Olaparib is used to treat a variety of BRCA-related tumors, including ovarian, breast, pancreatic and prostate cancer.

Olaparib is a PARPinhibitor, although it acts on PARP1, PARP2 and PARP3, olaparib It is a more selective NADcompetitive inhibitor+ at the catalytic site of PARP1 and PARP2. Inhibition of the BER pathway by olaparib results in the accumulation of unrepaired SSBs, leading to the formation of DSBs which are the most toxic form of DNA damage. Although BRCA-dependent homologous recombination can repair DSBs in normal cells, this repair pathway is defective in cells with BRCA1/2 mutations, such as certain tumor cells. Inhibition of PARP in cancer cells with BRCA mutations leads to genomic instability and apoptotic cell death. This end result is also known as synthetic lethality, a phenomenon that is the combination of two defects: inhibition of PARP activity and loss of DSB repair by HR-It is benign when used alone but can cause harmful results. In vitro studies suggest that olaparib-induced cytotoxicity may involve inhibition of PARP enzyme activity and increased formation of PARP-DNA complexes, leading to DNA damage and cancer cell death. If you want to get more high-quality information, you can contact Yaode, and Yaode will do its best to learn more about high-quality overseas drugs for you.