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Page 1
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
Currie KS, Kropf JE, Lee T, Blomgren P, Xu J, Zhao Z, Gallion S, Whitney JA, Maclin D, Lansdon EB, Maciejewski P, Rossi AM, Rong H, Macaluso J, Barbosa J, Di Paolo JA, Mitchell SA. Currie KS, et al. Among authors: maciejewski p. J Med Chem. 2014 May 8;57(9):3856-73. doi: 10.1021/jm500228a. Epub 2014 Apr 29. J Med Chem. 2014. PMID: 24779514
Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.
Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Gallion S, Hymowitz SG, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Maurer B, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Sowell CG, Wang X, Wong H, Xiong JM, Xu J, Zhao Z, Currie KS. Young WB, et al. Among authors: maciejewski p. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1333-7. doi: 10.1016/j.bmcl.2015.01.032. Epub 2015 Feb 7. Bioorg Med Chem Lett. 2015. PMID: 25701252
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.
Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Eigenbrot C, Gallion S, Johnson AR, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Wang X, Wong H, Xiong JM, Xu J, Yu C, Zhao Z, Currie KS. Young WB, et al. Among authors: maciejewski p. Bioorg Med Chem Lett. 2016 Jan 15;26(2):575-579. doi: 10.1016/j.bmcl.2015.11.076. Epub 2015 Nov 24. Bioorg Med Chem Lett. 2016. PMID: 26675441
Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.
Wang X, Barbosa J, Blomgren P, Bremer MC, Chen J, Crawford JJ, Deng W, Dong L, Eigenbrot C, Gallion S, Hau J, Hu H, Johnson AR, Katewa A, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, DiPaolo J, Reif K, Scheerens H, Schmitt A, Wong H, Xiong JM, Xu J, Zhao Z, Zhou F, Currie KS, Young WB. Wang X, et al. Among authors: maciejewski p. ACS Med Chem Lett. 2017 May 3;8(6):608-613. doi: 10.1021/acsmedchemlett.7b00103. eCollection 2017 Jun 8. ACS Med Chem Lett. 2017. PMID: 28626519 Free PMC article.
Imidazo[1,2-a]pyrazine diaryl ureas: inhibitors of the receptor tyrosine kinase EphB4.
Mitchell SA, Danca MD, Blomgren PA, Darrow JW, Currie KS, Kropf JE, Lee SH, Gallion SL, Xiong JM, Pippin DA, DeSimone RW, Brittelli DR, Eustice DC, Bourret A, Hill-Drzewi M, Maciejewski PM, Elkin LL. Mitchell SA, et al. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6991-5. doi: 10.1016/j.bmcl.2009.10.037. Epub 2009 Oct 15. Bioorg Med Chem Lett. 2009. PMID: 19879134
Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis.
Di Paolo JA, Huang T, Balazs M, Barbosa J, Barck KH, Bravo BJ, Carano RA, Darrow J, Davies DR, DeForge LE, Diehl L, Ferrando R, Gallion SL, Giannetti AM, Gribling P, Hurez V, Hymowitz SG, Jones R, Kropf JE, Lee WP, Maciejewski PM, Mitchell SA, Rong H, Staker BL, Whitney JA, Yeh S, Young WB, Yu C, Zhang J, Reif K, Currie KS. Di Paolo JA, et al. Among authors: maciejewski pm. Nat Chem Biol. 2011 Jan;7(1):41-50. doi: 10.1038/nchembio.481. Epub 2010 Nov 28. Nat Chem Biol. 2011. PMID: 21113169
Momelotinib inhibits ACVR1/ALK2, decreases hepcidin production, and ameliorates anemia of chronic disease in rodents.
Asshoff M, Petzer V, Warr MR, Haschka D, Tymoszuk P, Demetz E, Seifert M, Posch W, Nairz M, Maciejewski P, Fowles P, Burns CJ, Smith G, Wagner KU, Weiss G, Whitney JA, Theurl I. Asshoff M, et al. Among authors: maciejewski p. Blood. 2017 Mar 30;129(13):1823-1830. doi: 10.1182/blood-2016-09-740092. Epub 2017 Feb 10. Blood. 2017. PMID: 28188131 Free PMC article.
194 results