MK-4827(Niraparib) is a selective inhibitor of PARP1/PARP2 with IC50 of 3.8 nM/2.1 nM;with great activity in cancer cells with mutant BRCA-1 and BRCA-2;>330-fold selective against PARP3,V-PARP and Tank1.
1.Bryant HE, Schultz N, Thomas HD, Parker KM, Flower D, Lopez E, Kyle S, Meuth M, Curtin NJ, Helleday T. (2005) Specific killing of BRCA2-deficient tumours with inhibitors of poly(ADP-ribose) polymerase.. Nature, 434 (7035):(913-7). [PMID:15829966]
2.Farmer H, McCabe N, Lord CJ, Tutt AN, Johnson DA, Richardson TB, Santarosa M, Dillon KJ, Hickson I, Knights C et al.. (2005) Targeting the DNA repair defect in BRCA mutant cells as a therapeutic strategy.. Nature, 434 (7035):(917-21). [PMID:15829967]
3.Fong PC, Boss DS, Yap TA, Tutt A, Wu P, Mergui-Roelvink M, Mortimer P, Swaisland H, Lau A, O'Connor MJ et al.. (2009) Inhibition of poly(ADP-ribose) polymerase in tumors from BRCA mutation carriers.. N Engl J Med, 361 (2):(123-34). [PMID:19553641]
4.Jones P, Altamura S, Boueres J, Ferrigno F, Fonsi M, Giomini C, Lamartina S, Monteagudo E, Ontoria JM, Orsale MV et al.. (2009) Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.. J Med Chem, 52 (22):(7170-85). [PMID:19873981]
5.Reinbolt RE, Hays JL. (2013) The Role of PARP Inhibitors in the Treatment of Gynecologic Malignancies.. Front Oncol, 3 (3):(237). [PMID:24098868]
6.Murai J, Huang SY, Das BB, Renaud A, Zhang Y, Doroshow JH, Ji J, Takeda S, Pommier Y. (2012) Trapping of PARP1 and PARP2 by Clinical PARP Inhibitors.. Cancer Res, 72 (21):(5588-99). [PMID:23118055]
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