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Page 1
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Among authors: jaworski jp. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.
Gilmartin AG, Faitg TH, Richter M, Groy A, Seefeld MA, Darcy MG, Peng X, Federowicz K, Yang J, Zhang SY, Minthorn E, Jaworski JP, Schaber M, Martens S, McNulty DE, Sinnamon RH, Zhang H, Kirkpatrick RB, Nevins N, Cui G, Pietrak B, Diaz E, Jones A, Brandt M, Schwartz B, Heerding DA, Kumar R. Gilmartin AG, et al. Among authors: jaworski jp. Nat Chem Biol. 2014 Mar;10(3):181-7. doi: 10.1038/nchembio.1427. Epub 2014 Jan 5. Nat Chem Biol. 2014. PMID: 24390428
Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists.
Hilfiker MA, Wang N, Hou X, Du Z, Pullen MA, Nord M, Nagilla R, Fries HE, Wu CW, Sulpizio AC, Jaworski JP, Morrow D, Edwards RM, Jin J. Hilfiker MA, et al. Among authors: jaworski jp. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4292-5. doi: 10.1016/j.bmcl.2009.05.074. Epub 2009 May 27. Bioorg Med Chem Lett. 2009. PMID: 19487124
Structure-activity relationship studies of novel 3-oxazolidinedione-6-naphthyl-2-pyridinones as potent and orally bioavailable EP3 receptor antagonists.
Morales-Ramos ÁI, Li YH, Hilfiker M, Mecom JS, Eidam P, Shi D, Tseng PS, Brooks C, Zhang D, Wang N, Jaworski JP, Morrow D, Fries H, Edwards R, Jin J. Morales-Ramos ÁI, et al. Among authors: jaworski jp. Bioorg Med Chem Lett. 2011 May 15;21(10):2806-11. doi: 10.1016/j.bmcl.2011.03.107. Epub 2011 Apr 5. Bioorg Med Chem Lett. 2011. PMID: 21514150
Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.
Jin J, Morales-Ramos A, Eidam P, Mecom J, Li Y, Brooks C, Hilfiker M, Zhang D, Wang N, Shi D, Tseng PS, Wheless K, Budzik B, Evans K, Jaworski JP, Jugus J, Leon L, Wu C, Pullen M, Karamshi B, Rao P, Ward E, Laping N, Evans C, Leach C, Holt D, Su X, Morrow D, Fries H, Thorneloe K, Edwards R. Jin J, et al. Among authors: jaworski jp. ACS Med Chem Lett. 2010 May 14;1(7):316-20. doi: 10.1021/ml100077x. eCollection 2010 Oct 14. ACS Med Chem Lett. 2010. PMID: 24900213 Free PMC article.
37 results