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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: zarrin aa. 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
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: zarrin aa. 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.
TPL2 kinase action and control of inflammation.
Xu D, Matsumoto ML, McKenzie BS, Zarrin AA. Xu D, et al. Among authors: zarrin aa. 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.
Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.
Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z. Burch JD, et al. Among authors: zarrin aa. J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27. J Med Chem. 2014. PMID: 24918870
Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.
Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF, Zarrin AA, McEwan PA, Barker JJ, Ellebrandt C, Kordt D, Stein DB, Wang X, Chen Y, Hu B, Xu X, Yuen PW, Zhang Y, Pei Z. Burch JD, et al. Among authors: zarrin aa. J Med Chem. 2015 May 14;58(9):3806-16. doi: 10.1021/jm501998m. Epub 2015 Apr 16. J Med Chem. 2015. PMID: 25844760
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: zarrin aa. Sci Signal. 2017 Apr 18;10(475):eaah4273. doi: 10.1126/scisignal.aah4273. Sci Signal. 2017. PMID: 28420753
Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).
Trani G, Barker JJ, Bromidge SM, Brookfield FA, Burch JD, Chen Y, Eigenbrot C, Heifetz A, Ismaili MHA, Johnson A, Krülle TM, MacKinnon CH, Maghames R, McEwan PA, Montalbetti CAGN, Ortwine DF, Pérez-Fuertes Y, Vaidya DG, Wang X, Zarrin AA, Pei Z. Trani G, et al. Among authors: zarrin aa. Bioorg Med Chem Lett. 2014 Dec 15;24(24):5818-5823. doi: 10.1016/j.bmcl.2014.10.020. Epub 2014 Oct 12. Bioorg Med Chem Lett. 2014. PMID: 25455497
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: zarrin aa. Sci Signal. 2015 Dec 1;8(405):ra122. doi: 10.1126/scisignal.aab0949. Sci Signal. 2015. PMID: 26628680
Evolutionarily conserved paired immunoglobulin-like receptor α (PILRα) domain mediates its interaction with diverse sialylated ligands.
Sun Y, Senger K, Baginski TK, Mazloom A, Chinn Y, Pantua H, Hamidzadeh K, Ramani SR, Luis E, Tom I, Sebrell A, Quinones G, Ma Y, Mukhyala K, Sai T, Ding J, Haley B, Shadnia H, Kapadia SB, Gonzalez LC, Hass PE, Zarrin AA. Sun Y, et al. Among authors: zarrin aa. J Biol Chem. 2012 May 4;287(19):15837-50. doi: 10.1074/jbc.M111.286633. Epub 2012 Mar 6. J Biol Chem. 2012. PMID: 22396535 Free PMC article.
Function of CSF1 and IL34 in Macrophage Homeostasis, Inflammation, and Cancer.
Lin W, Xu D, Austin CD, Caplazi P, Senger K, Sun Y, Jeet S, Young J, Delarosa D, Suto E, Huang Z, Zhang J, Yan D, Corzo C, Barck K, Rajan S, Looney C, Gandham V, Lesch J, Liang WC, Mai E, Ngu H, Ratti N, Chen Y, Misner D, Lin T, Danilenko D, Katavolos P, Doudemont E, Uppal H, Eastham J, Mak J, de Almeida PE, Bao K, Hadadianpour A, Keir M, Carano RAD, Diehl L, Xu M, Wu Y, Weimer RM, DeVoss J, Lee WP, Balazs M, Walsh K, Alatsis KR, Martin F, Zarrin AA. Lin W, et al. Among authors: zarrin aa. Front Immunol. 2019 Sep 4;10:2019. doi: 10.3389/fimmu.2019.02019. eCollection 2019. Front Immunol. 2019. PMID: 31552020 Free PMC article.
45 results