REVIEW Olaparib is a small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. It selectively binds to and inhibits PARP. The inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. It acts against cancers in people with hereditary BRCA1 or BRCA2 mutations, which includes many ovarian, breast and prostate cancers.
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Vasiliou, S.; Castaner, R.; Bolos, J. Olaparib: PARP-1 and PARP-2 inhibitor oncolytic. Drugs of the Future. (2009) 34(2): 101-105.
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Chen, Ying; Zhang, Lei; Hao, Quan. Olaparib: a promising PARP inhibitor in ovarian cancer therapy. Archives of Gynecology and Obstetrics. (2013) 288(2): 367-374.
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Menear, Keith A.; Adcock, Claire; Boulter, Robert; Cockcroft, Xiao-ling; Copsey, Louise; Cranston, Aaron; Dillon, Krystyna J.; Drzewiecki, Jan; Garman, Sheila; Gomez, Sylvie; et al. 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1. Journal of Medicinal Chemistry. (2008) 51(20): 6581-6591
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Martin, Niall Morrison Barr; Smith, Graeme Cameron Murray; Jackson, Stephen Philip; Loh, Vincent M., Jr.; Cockcroft, Xiao-Ling Fan; Matthews, Ian Timothy Williams; Menear, Keith Allan; Kerrigan, Frank; Ashworth, AlanPreparation of phthalazinones as PARP inhibitors PCT Int. Appl. (2004), WO 2004080976 A1 20040923.
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