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Page 1
Bruton's Tyrosine Kinase Small Molecule Inhibitors Induce a Distinct Pancreatic Toxicity in Rats.
Erickson RI, Schutt LK, Tarrant JM, McDowell M, Liu L, Johnson AR, Lewin-Koh SC, Hedehus M, Ross J, Carano RA, Staflin K, Zhong F, Crawford JJ, Zhong S, Reif K, Katewa A, Wong H, Young WB, Dambach DM, Misner DL. Erickson RI, et al. Among authors: reif k. J Pharmacol Exp Ther. 2017 Jan;360(1):226-238. doi: 10.1124/jpet.116.236224. Epub 2016 Nov 7. J Pharmacol Exp Ther. 2017. PMID: 27821712
Antiarthritis effect of a novel Bruton's tyrosine kinase (BTK) inhibitor in rat collagen-induced arthritis and mechanism-based pharmacokinetic/pharmacodynamic modeling: relationships between inhibition of BTK phosphorylation and efficacy.
Liu L, Di Paolo J, Barbosa J, Rong H, Reif K, Wong H. Liu L, et al. Among authors: reif k. J Pharmacol Exp Ther. 2011 Jul;338(1):154-63. doi: 10.1124/jpet.111.181545. Epub 2011 Apr 26. J Pharmacol Exp Ther. 2011. PMID: 21521773
Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.
Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB. Crawford JJ, et al. Among authors: reif k. J Med Chem. 2018 Mar 22;61(6):2227-2245. doi: 10.1021/acs.jmedchem.7b01712. Epub 2018 Feb 23. J Med Chem. 2018. PMID: 29457982
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: reif k. 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
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: reif k. 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 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: reif k. 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.
Stereochemical Differences in Fluorocyclopropyl Amides Enable Tuning of Btk Inhibition and Off-Target Activity.
Crawford JJ, Lee W, Johnson AR, Delatorre KJ, Chen J, Eigenbrot C, Heidmann J, Kakiuchi-Kiyota S, Katewa A, Kiefer JR, Liu L, Lubach JW, Misner D, Purkey H, Reif K, Vogt J, Wong H, Yu C, Young WB. Crawford JJ, et al. Among authors: reif k. ACS Med Chem Lett. 2020 Jul 13;11(8):1588-1597. doi: 10.1021/acsmedchemlett.0c00249. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832028 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: reif k. JCI Insight. 2017 Apr 6;2(7):e90111. doi: 10.1172/jci.insight.90111. JCI Insight. 2017. PMID: 28405610 Free PMC article.
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: reif k. Nat Chem Biol. 2011 Jan;7(1):41-50. doi: 10.1038/nchembio.481. Epub 2010 Nov 28. Nat Chem Biol. 2011. PMID: 21113169
Preclinical Safety Profile of a Depleting Antibody against CRTh2 for Asthma: Well Tolerated Despite Unexpected CRTh2 Expression on Vascular Pericytes in the Central Nervous System and Gastric Mucosa.
Rajapaksa KS, Huang T, Sharma N, Liu S, Solon M, Reyes A, Paul S, Yee A, Tao J, Chalasani S, Bien-Ly N, Barck K, Carano RA, Wang J, Rangell L, Bremer M, Danilenko DM, Katavolos P, Hotzel I, Reif K, Austin CD. Rajapaksa KS, et al. Among authors: reif k. Toxicol Sci. 2016 Jul;152(1):72-84. doi: 10.1093/toxsci/kfw067. Epub 2016 Apr 21. Toxicol Sci. 2016. PMID: 27103662
112 results