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Page 1
Discovery of Potent Benzolactam IRAK4 Inhibitors with Robust in Vivo Activity.
Rajapaksa NS, Gobbi A, Drobnick J, Do S, Kolesnikov A, Liang J, Chen Y, Sujatha-Bhaskar S, Huang Z, Brightbill H, Francis R, Yu C, Choo EF, DeMent K, Ran Y, An L, Emson C, Maher J, Wai J, McKenzie BS, Lupardus PJ, Zarrin AA, Kiefer JR, Bryan MC. Rajapaksa NS, et al. Among authors: bryan mc. ACS Med Chem Lett. 2019 Nov 11;11(3):327-333. doi: 10.1021/acsmedchemlett.9b00380. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184965 Free PMC article.
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Nishimura N, Siegmund A, Liu L, Yang K, Bryan MC, Andrews KL, Bo Y, Booker SK, Caenepeel S, Freeman D, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Whittington DA, Zalameda L, Zhang N, Hughes PE, Norman MH. Nishimura N, et al. Among authors: bryan mc. J Med Chem. 2011 Jul 14;54(13):4735-51. doi: 10.1021/jm200386s. Epub 2011 Jun 20. J Med Chem. 2011. PMID: 21612232
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.
Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Tam C, Wang S, Yeap SK, Yen I, Yin J, Yu C, Zilberleyb I, Heffron TP. Hanan EJ, et al. Among authors: bryan mc. J Med Chem. 2014 Dec 11;57(23):10176-91. doi: 10.1021/jm501578n. Epub 2014 Nov 20. J Med Chem. 2014. PMID: 25383627 Free PMC article.
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, Heffron TP. Hanan EJ, et al. Among authors: bryan mc. Bioorg Med Chem Lett. 2016 Jan 15;26(2):534-539. doi: 10.1016/j.bmcl.2015.11.078. Epub 2015 Nov 22. Bioorg Med Chem Lett. 2016. PMID: 26639762
Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.
Bryan MC, Burdick DJ, Chan BK, Chen Y, Clausen S, Dotson J, Eigenbrot C, Elliott R, Hanan EJ, Heald R, Jackson P, La H, Lainchbury M, Malek S, Mann SE, Purkey HE, Schaefer G, Schmidt S, Seward E, Sideris S, Wang S, Yen I, Yu C, Heffron TP. Bryan MC, et al. ACS Med Chem Lett. 2015 Dec 17;7(1):100-4. doi: 10.1021/acsmedchemlett.5b00428. eCollection 2016 Jan 14. ACS Med Chem Lett. 2015. PMID: 26819674 Free PMC article.
Development of Potent and Selective Pyrazolopyrimidine IRAK4 Inhibitors.
Bryan MC, Drobnick J, Gobbi A, Kolesnikov A, Chen Y, Rajapaksa N, Ndubaku C, Feng J, Chang W, Francis R, Yu C, Choo EF, DeMent K, Ran Y, An L, Emson C, Huang Z, Sujatha-Bhaskar S, Brightbill H, DiPasquale A, Maher J, Wai J, McKenzie BS, Lupardus PJ, Zarrin AA, Kiefer JR. Bryan MC, et al. J Med Chem. 2019 Jul 11;62(13):6223-6240. doi: 10.1021/acs.jmedchem.9b00439. Epub 2019 May 24. J Med Chem. 2019. PMID: 31082230
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: bryan mc. Sci Signal. 2020 Jun 2;13(634):eaaz1053. doi: 10.1126/scisignal.aaz1053. Sci Signal. 2020. PMID: 32487715
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
Zeng M, Grandner JM, Bryan MC, Verma V, Larouche-Gauthier R, Leclerc JP, Zhao L, Haghshenas P, Aubert-Nicol S, Yadav A, Ashley M, Chen JZ, Durk M, Samy KE, Nespi M, Levy E, Merrick K, Moffat JG, Murray J, Oh A, Orr C, Segal E, Sims J, Sneeringer C, Prangley M, Vartanian S, Magnuson S, Parr BT. Zeng M, et al. Among authors: bryan mc. ACS Med Chem Lett. 2023 Aug 24;14(9):1179-1187. doi: 10.1021/acsmedchemlett.3c00142. eCollection 2023 Sep 14. ACS Med Chem Lett. 2023. PMID: 37736184 Free PMC article.
36 results