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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: bremer mc. 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: bremer mc. 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
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. JCI Insight. 2017 Apr 6;2(7):e90111. doi: 10.1172/jci.insight.90111. JCI Insight. 2017. PMID: 28405610 Free PMC article.
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: bremer mc. 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.
Safety, Pharmacokinetics, and Pharmacodynamics in Healthy Volunteers Treated With GDC-0853, a Selective Reversible Bruton's Tyrosine Kinase Inhibitor.
Herman AE, Chinn LW, Kotwal SG, Murray ER, Zhao R, Florero M, Lin A, Moein A, Wang R, Bremer M, Kokubu S, Serone AP, Hanze EL, Viberg A, Morimoto AM, Winter HR, Katsumoto TR. Herman AE, et al. Clin Pharmacol Ther. 2018 Jun;103(6):1020-1028. doi: 10.1002/cpt.1056. Epub 2018 Mar 23. Clin Pharmacol Ther. 2018. PMID: 29484638 Clinical Trial.
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. Toxicol Sci. 2016 Jul;152(1):72-84. doi: 10.1093/toxsci/kfw067. Epub 2016 Apr 21. Toxicol Sci. 2016. PMID: 27103662
Dose-dependent inactivation of airway tryptase with a novel dissociating anti-tryptase antibody (MTPS9579A) in healthy participants: A randomized trial.
Rymut SM, Sukumaran S, Sperinde G, Bremer M, Galanter J, Yoshida K, Smith J, Banerjee P, Sverkos V, Cai F, Steffen V, Henderson LM, Rhee H, Belloni PN, Lin JH, Staton TL. Rymut SM, et al. Clin Transl Sci. 2022 Feb;15(2):451-463. doi: 10.1111/cts.13163. Epub 2021 Sep 30. Clin Transl Sci. 2022. PMID: 34581002 Free PMC article. Clinical Trial.
An Allosteric Anti-tryptase Antibody for the Treatment of Mast Cell-Mediated Severe Asthma.
Maun HR, Jackman JK, Choy DF, Loyet KM, Staton TL, Jia G, Dressen A, Hackney JA, Bremer M, Walters BT, Vij R, Chen X, Trivedi NN, Morando A, Lipari MT, Franke Y, Wu X, Zhang J, Liu J, Wu P, Chang D, Orozco LD, Christensen E, Wong M, Corpuz R, Hang JQ, Lutman J, Sukumaran S, Wu Y, Ubhayakar S, Liang X, Schwartz LB, Babina M, Woodruff PG, Fahy JV, Ahuja R, Caughey GH, Kusi A, Dennis MS, Eigenbrot C, Kirchhofer D, Austin CD, Wu LC, Koerber JT, Lee WP, Yaspan BL, Alatsis KR, Arron JR, Lazarus RA, Yi T. Maun HR, et al. Cell. 2019 Oct 3;179(2):417-431.e19. doi: 10.1016/j.cell.2019.09.009. Cell. 2019. PMID: 31585081 Free PMC article.
18 results