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Page 1
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. Among authors: mckenzie bs. 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
Scaffold-Hopping Approach To Discover Potent, Selective, and Efficacious Inhibitors of NF-κB Inducing Kinase.
Blaquiere N, Castanedo GM, Burch JD, Berezhkovskiy LM, Brightbill H, Brown S, Chan C, Chiang PC, Crawford JJ, Dong T, Fan P, Feng J, Ghilardi N, Godemann R, Gogol E, Grabbe A, Hole AJ, Hu B, Hymowitz SG, Alaoui Ismaili MH, Le H, Lee P, Lee W, Lin X, Liu N, McEwan PA, McKenzie B, Silvestre HL, Suto E, Sujatha-Bhaskar S, Wu G, Wu LC, Zhang Y, Zhong Z, Staben ST. Blaquiere N, et al. J Med Chem. 2018 Aug 9;61(15):6801-6813. doi: 10.1021/acs.jmedchem.8b00678. Epub 2018 Jul 24. J Med Chem. 2018. PMID: 29940120
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: mckenzie bs. 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.
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: mckenzie bs. Sci Signal. 2020 Jun 2;13(634):eaaz1053. doi: 10.1126/scisignal.aaz1053. Sci Signal. 2020. PMID: 32487715
TPL2 kinase action and control of inflammation.
Xu D, Matsumoto ML, McKenzie BS, Zarrin AA. Xu D, et al. Among authors: mckenzie bs. Pharmacol Res. 2018 Mar;129:188-193. doi: 10.1016/j.phrs.2017.11.031. Epub 2017 Nov 26. Pharmacol Res. 2018. PMID: 29183769 Free article. Review.
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: mckenzie bs. 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
The kinase TPL2 activates ERK and p38 signaling to promote neutrophilic inflammation.
Senger K, Pham VC, Varfolomeev E, Hackney JA, Corzo CA, Collier J, Lau VWC, Huang Z, Hamidzhadeh K, Caplazi P, Peng I, Setiadi AF, Francis R, Paler-Martinez A, Kwon YC, Ramirez-Carrozzi V, Sun Y, Grigg PW, Roose-Girma M, Jeet S, Barck KH, Pham A, Ota N, Ha C, Stinson J, Guillory J, Tam L, Modrusan Z, Emson C, McKenzie BS, Townsend MJ, Carano RAD, Warming S, Vucic D, DeVoss J, Lee WP, Lill JR, Zarrin AA. Senger K, et al. Among authors: mckenzie bs. Sci Signal. 2017 Apr 18;10(475):eaah4273. doi: 10.1126/scisignal.aah4273. Sci Signal. 2017. PMID: 28420753
NF-κB inducing kinase is a therapeutic target for systemic lupus erythematosus.
Brightbill HD, Suto E, Blaquiere N, Ramamoorthi N, Sujatha-Bhaskar S, Gogol EB, Castanedo GM, Jackson BT, Kwon YC, Haller S, Lesch J, Bents K, Everett C, Kohli PB, Linge S, Christian L, Barrett K, Jaochico A, Berezhkovskiy LM, Fan PW, Modrusan Z, Veliz K, Townsend MJ, DeVoss J, Johnson AR, Godemann R, Lee WP, Austin CD, McKenzie BS, Hackney JA, Crawford JJ, Staben ST, Alaoui Ismaili MH, Wu LC, Ghilardi N. Brightbill HD, et al. Among authors: mckenzie bs. Nat Commun. 2018 Jan 12;9(1):179. doi: 10.1038/s41467-017-02672-0. Nat Commun. 2018. PMID: 29330524 Free PMC article.
RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Patel S, Webster JD, Varfolomeev E, Kwon YC, Cheng JH, Zhang J, Dugger DL, Wickliffe KE, Maltzman A, Sujatha-Bhaskar S, Bir Kohli P, Ramaswamy S, Deshmukh G, Liederer BM, Fong R, Hamilton G, Lupardus P, Caplazi P, Lee WP, van Lookeren Campagne M, Johnson A, McKenzie BS, Junttila MR, Newton K, Vucic D. Patel S, et al. Among authors: mckenzie bs. Cell Death Differ. 2020 Jan;27(1):161-175. doi: 10.1038/s41418-019-0347-0. Epub 2019 May 17. Cell Death Differ. 2020. PMID: 31101885 Free PMC article.
Inhibition of the kinase ITK in a mouse model of asthma reduces cell death and fails to inhibit the inflammatory response.
Sun Y, Peng I, Webster JD, Suto E, Lesch J, Wu X, Senger K, Francis G, Barrett K, Collier JL, Burch JD, Zhou M, Chen Y, Chan C, Eastham-Anderson J, Ngu H, Li O, Staton T, Havnar C, Jaochico A, Jackman J, Jeet S, Riol-Blanco L, Wu LC, Choy DF, Arron JR, McKenzie BS, Ghilardi N, Ismaili MH, Pei Z, DeVoss J, Austin CD, Lee WP, Zarrin AA. Sun Y, et al. Among authors: mckenzie bs. Sci Signal. 2015 Dec 1;8(405):ra122. doi: 10.1126/scisignal.aab0949. Sci Signal. 2015. PMID: 26628680
57 results