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Page 1
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: blomgren 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 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: blomgren 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
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: blomgren 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: blomgren 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
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Farand J, Kropf JE, Blomgren P, Xu J, Schmitt AC, Newby ZE, Wang T, Murakami E, Barauskas O, Sudhamsu J, Feng JY, Niedziela-Majka A, Schultz BE, Schwartz K, Viatchenko-Karpinski S, Kornyeyev D, Kashishian A, Fan P, Chen X, Lansdon EB, Ports MO, Currie KS, Watkins WJ, Notte GT. Farand J, et al. Among authors: blomgren p. ACS Med Chem Lett. 2019 Nov 19;11(3):358-364. doi: 10.1021/acsmedchemlett.9b00420. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184970 Free PMC article.
Discovery of Lanraplenib (GS-9876): A Once-Daily Spleen Tyrosine Kinase Inhibitor for Autoimmune Diseases.
Blomgren P, Chandrasekhar J, Di Paolo JA, Fung W, Geng G, Ip C, Jones R, Kropf JE, Lansdon EB, Lee S, Lo JR, Mitchell SA, Murray B, Pohlmeyer C, Schmitt A, Suekawa-Pirrone K, Wise S, Xiong JM, Xu J, Yu H, Zhao Z, Currie KS. Blomgren P, et al. ACS Med Chem Lett. 2020 Feb 12;11(4):506-513. doi: 10.1021/acsmedchemlett.9b00621. eCollection 2020 Apr 9. ACS Med Chem Lett. 2020. PMID: 32292557 Free PMC article.
Btk-specific inhibition blocks pathogenic plasma cell signatures and myeloid cell-associated damage in IFNα-driven lupus nephritis.
Katewa A, Wang Y, Hackney JA, Huang T, Suto E, Ramamoorthi N, Austin CD, Bremer M, Chen JZ, Crawford JJ, Currie KS, Blomgren P, DeVoss J, DiPaolo JA, Hau J, Johnson A, Lesch J, DeForge LE, Lin Z, Liimatta M, Lubach JW, McVay S, Modrusan Z, Nguyen A, Poon C, Wang J, Liu L, Lee WP, Wong H, Young WB, Townsend MJ, Reif K. Katewa A, et al. Among authors: blomgren p. JCI Insight. 2017 Apr 6;2(7):e90111. doi: 10.1172/jci.insight.90111. JCI Insight. 2017. PMID: 28405610 Free PMC article.
Design, synthesis, and antiviral properties of 4'-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479.
Smith DB, Martin JA, Klumpp K, Baker SJ, Blomgren PA, Devos R, Granycome C, Hang J, Hobbs CJ, Jiang WR, Laxton C, Le Pogam S, Leveque V, Ma H, Maile G, Merrett JH, Pichota A, Sarma K, Smith M, Swallow S, Symons J, Vesey D, Najera I, Cammack N. Smith DB, et al. Bioorg Med Chem Lett. 2007 May 1;17(9):2570-6. doi: 10.1016/j.bmcl.2007.02.004. Epub 2007 Feb 4. Bioorg Med Chem Lett. 2007. PMID: 17317178
50 results