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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: osterling dj. 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
The Histone Methyltransferase Inhibitor A-366 Uncovers a Role for G9a/GLP in the Epigenetics of Leukemia.
Pappano WN, Guo J, He Y, Ferguson D, Jagadeeswaran S, Osterling DJ, Gao W, Spence JK, Pliushchev M, Sweis RF, Buchanan FG, Michaelides MR, Shoemaker AR, Tse C, Chiang GG. Pappano WN, et al. Among authors: osterling dj. PLoS One. 2015 Jul 6;10(7):e0131716. doi: 10.1371/journal.pone.0131716. eCollection 2015. PLoS One. 2015. PMID: 26147105 Free PMC article.
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: osterling dj. 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: osterling dj. 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: osterling dj. 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: osterling dj. 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.
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