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Olaparib.

Recent Results Cancer Res

November 2018

Cancer Center Heilbronn-Franken, SLK-Kliniken Heilbronn GmbH and MOLIT Institute for Personalized Medicine, Am Gesundbrunnen 20-24, 74078, Heilbronn, Germany.

Olaparib (Lynparza [AstraZeneca, Cambridge, UK], formerly referred to as AZD2281 or KU0059436) is an oral poly(ADP-ribose) polymerase (PARP) inhibitor. It is rationally designed to act as a competitive inhibitor of NAD at the catalytic site of PARP1 and PARP2, both members of the PARP family of enzymes that are central to the repair of DNA single-strand breaks (SSBs) mediated via the base excision repair (BER) pathway. Inhibition of the BER pathway by olaparib leads to the accumulation of unrepaired SSBs, which leads to the formation of deleterious double-strand breaks (DSBs).

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