Olaparib (AZD2281, KU0059436, AZD-2281, KU-0059436),又称奥拉帕尼或奥拉帕利,是一种可口服的PARP1/2抑制剂,IC50分别为5和1 nM,破坏PARP介导DNA修复机制,诱导细胞凋亡,表现出抗肿瘤活性。
参考文献
1.Menear KA, et al. 4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1. J Med Chem. 2008 Oct 23;51(20):6581-91.
2.Rottenberg S, et al. High sensitivity of BRCA1-deficient mammary tumors to the PARP inhibitor AZD2281 alone and in combination with platinum drugs. Proc Natl Acad Sci U S A. 2008 Nov 4;105(44):17079-84.
3.Bian X, et al. PTEN deficiency sensitizes endometrioid endometrial cancer to compound PARP-PI3K inhibition but not PARP inhibition as monotherapy. Oncogene. 2018 Jan 18;37(3):341-351.
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