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Page 1
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
McBride C, Trzoss L, Povero D, Lazic M, Ambrus-Aikelin G, Santini A, Pranadinata R, Bain G, Stansfield R, Stafford JA, Veal J, Takahashi R, Ly J, Chen S, Liu L, Nespi M, Blake R, Katewa A, Kleinheinz T, Sujatha-Bhaskar S, Ramamoorthi N, Sims J, McKenzie B, Chen M, Ultsch M, Johnson M, Murray J, Ciferri C, Staben ST, Townsend MJ, Stivala CE. McBride C, et al. Among authors: katewa a. J Med Chem. 2022 Nov 10;65(21):14721-14739. doi: 10.1021/acs.jmedchem.2c01250. Epub 2022 Oct 24. J Med Chem. 2022. PMID: 36279149
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: katewa a. 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
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: katewa a. 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. 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: katewa a. 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.
The kinase IRAK4 promotes endosomal TLR and immune complex signaling in B cells and plasmacytoid dendritic cells.
Corzo CA, Varfolomeev E, Setiadi AF, Francis R, Klabunde S, Senger K, Sujatha-Bhaskar S, Drobnick J, Do S, Suto E, Huang Z, Eastham-Anderson J, Katewa A, Pang J, Domeyer M, Dela Cruz C, Paler-Martinez A, Lau VWC, Hadadianpour A, Ramirez-Carrozi V, Sun Y, Bao K, Xu D, Hunley E, Brightbill HD, Warming S, Roose-Girma M, Wong A, Tam L, Emson CL, Crawford JJ, Young WB, Pappu R, McKenzie BS, Asghari V, Vucic D, Hackney JA, Austin CD, Lee WP, Lekkerkerker A, Ghilardi N, Bryan MC, Kiefer JR, Townsend MJ, Zarrin AA. Corzo CA, et al. Among authors: katewa a. Sci Signal. 2020 Jun 2;13(634):eaaz1053. doi: 10.1126/scisignal.aaz1053. Sci Signal. 2020. PMID: 32487715
Depletion of major pathogenic cells in asthma by targeting CRTh2.
Huang T, Hazen M, Shang Y, Zhou M, Wu X, Yan D, Lin Z, Solon M, Luis E, Ngu H, Shi Y, Katewa A, Choy DF, Ramamoorthi N, Castellanos ER, Balazs M, Xu M, Lee WP, Matsumoto ML, Payandeh J, Arron JR, Hongo JA, Wang J, Hötzel I, Austin CD, Reif K. Huang T, et al. Among authors: katewa a. JCI Insight. 2016 May 19;1(7):e86689. doi: 10.1172/jci.insight.86689. JCI Insight. 2016. PMID: 27699264 Free PMC article.
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: katewa a. 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
Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations.
Johnson AR, Kohli PB, Katewa A, Gogol E, Belmont LD, Choy R, Penuel E, Burton L, Eigenbrot C, Yu C, Ortwine DF, Bowman K, Franke Y, Tam C, Estevez A, Mortara K, Wu J, Li H, Lin M, Bergeron P, Crawford JJ, Young WB. Johnson AR, et al. Among authors: katewa a. ACS Chem Biol. 2016 Oct 21;11(10):2897-2907. doi: 10.1021/acschembio.6b00480. Epub 2016 Sep 7. ACS Chem Biol. 2016. PMID: 27571029
43 results