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Page 1
Mechanistic Dissection of PARP1 Trapping and the Impact on In Vivo Tolerability and Efficacy of PARP Inhibitors.
Hopkins TA, Shi Y, Rodriguez LE, Solomon LR, Donawho CK, DiGiammarino EL, Panchal SC, Wilsbacher JL, Gao W, Olson AM, Stolarik DF, Osterling DJ, Johnson EF, Maag D. Hopkins TA, et al. Among authors: olson am. Mol Cancer Res. 2015 Nov;13(11):1465-77. doi: 10.1158/1541-7786.MCR-15-0191-T. Epub 2015 Jul 27. Mol Cancer Res. 2015. PMID: 26217019 Free article.
ABT-888, an orally active poly(ADP-ribose) polymerase inhibitor that potentiates DNA-damaging agents in preclinical tumor models.
Donawho CK, Luo Y, Luo Y, Penning TD, Bauch JL, Bouska JJ, Bontcheva-Diaz VD, Cox BF, DeWeese TL, Dillehay LE, Ferguson DC, Ghoreishi-Haack NS, Grimm DR, Guan R, Han EK, Holley-Shanks RR, Hristov B, Idler KB, Jarvis K, Johnson EF, Kleinberg LR, Klinghofer V, Lasko LM, Liu X, Marsh KC, McGonigal TP, Meulbroek JA, Olson AM, Palma JP, Rodriguez LE, Shi Y, Stavropoulos JA, Tsurutani AC, Zhu GD, Rosenberg SH, Giranda VL, Frost DJ. Donawho CK, et al. Among authors: olson am. Clin Cancer Res. 2007 May 1;13(9):2728-37. doi: 10.1158/1078-0432.CCR-06-3039. Clin Cancer Res. 2007. PMID: 17473206
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Penning TD, et al. Among authors: olson am. J Med Chem. 2009 Jan 22;52(2):514-23. doi: 10.1021/jm801171j. J Med Chem. 2009. PMID: 19143569
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.
Tong Y, Bouska JJ, Ellis PA, Johnson EF, Leverson J, Liu X, Marcotte PA, Olson AM, Osterling DJ, Przytulinska M, Rodriguez LE, Shi Y, Soni N, Stavropoulos J, Thomas S, Donawho CK, Frost DJ, Luo Y, Giranda VL, Penning TD. Tong Y, et al. Among authors: olson am. J Med Chem. 2009 Nov 12;52(21):6803-13. doi: 10.1021/jm900697r. J Med Chem. 2009. PMID: 19888760
Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor.
Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Penning TD, et al. Among authors: olson am. J Med Chem. 2010 Apr 22;53(8):3142-53. doi: 10.1021/jm901775y. J Med Chem. 2010. PMID: 20337371
Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.
Tong Y, Torrent M, Florjancic AS, Bromberg KD, Buchanan FG, Ferguson DC, Johnson EF, Lasko LM, Maag D, Merta PJ, Olson AM, Osterling DJ, Soni N, Shoemaker AR, Penning TD. Tong Y, et al. Among authors: olson am. ACS Med Chem Lett. 2014 Aug 6;6(1):58-62. doi: 10.1021/ml5002745. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589931 Free PMC article.
The PARP inhibitor, ABT-888 potentiates temozolomide: correlation with drug levels and reduction in PARP activity in vivo.
Palma JP, Rodriguez LE, Bontcheva-Diaz VD, Bouska JJ, Bukofzer G, Colon-Lopez M, Guan R, Jarvis K, Johnson EF, Klinghofer V, Liu X, Olson A, Saltarelli MJ, Shi Y, Stavropoulos JA, Zhu GD, Penning TD, Luo Y, Giranda VL, Rosenberg SH, Frost DJ, Donawho CK. Palma JP, et al. Anticancer Res. 2008 Sep-Oct;28(5A):2625-35. Anticancer Res. 2008. PMID: 19035287 Free article.
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Penning TD, Zhu GD, Gandhi VB, Gong J, Thomas S, Lubisch W, Grandel R, Wernet W, Park CH, Fry EH, Liu X, Shi Y, Klinghofer V, Johnson EF, Donawho CK, Frost DJ, Bontcheva-Diaz V, Bouska JJ, Olson AM, Marsh KC, Luo Y, Rosenberg SH, Giranda VL. Penning TD, et al. Among authors: olson am. Bioorg Med Chem. 2008 Jul 15;16(14):6965-75. doi: 10.1016/j.bmc.2008.05.044. Epub 2008 May 27. Bioorg Med Chem. 2008. PMID: 18541433
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