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Page 1
3,5-Disubstituted-indole-7-carboxamides as IKKβ Inhibitors: Optimization of Oral Activity via the C3 Substituent.
Kerns JK, Busch-Petersen J, Fu W, Boehm JC, Nie H, Muratore M, Bullion A, Lin G, Li H, Davis R, Lin X, Lakdawala AS, Cousins R, Field R, Payne J, Miller DD, Bamborough P, Christopher JA, Baldwin I, Osborn RR, Yonchuk J, Webb E, Rumsey WL. Kerns JK, et al. Among authors: yonchuk j. ACS Med Chem Lett. 2018 Oct 30;9(12):1164-1169. doi: 10.1021/acsmedchemlett.8b00291. eCollection 2018 Dec 13. ACS Med Chem Lett. 2018. PMID: 30613320 Free PMC article.
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Davies TG, Wixted WE, Coyle JE, Griffiths-Jones C, Hearn K, McMenamin R, Norton D, Rich SJ, Richardson C, Saxty G, Willems HM, Woolford AJ, Cottom JE, Kou JP, Yonchuk JG, Feldser HG, Sanchez Y, Foley JP, Bolognese BJ, Logan G, Podolin PL, Yan H, Callahan JF, Heightman TD, Kerns JK. Davies TG, et al. Among authors: yonchuk jg. J Med Chem. 2016 Apr 28;59(8):3991-4006. doi: 10.1021/acs.jmedchem.6b00228. Epub 2016 Apr 12. J Med Chem. 2016. PMID: 27031670
Discovery of a crystalline sulforaphane analog with good solid-state stability and engagement of the Nrf2 pathway in vitro and in vivo.
Boehm J, Davis R, Murar CE, Li T, McCleland B, Dong S, Yan H, Kerns J, Moody CJ, Wilson AJ, Graves AP, Mentzer M, Qi H, Yonchuk J, Kou JP, Foley J, Sanchez Y, Podolin PL, Bolognese B, Booth-Genthe C, Galop M, Wolfe L, Carr R, Callahan JF. Boehm J, et al. Among authors: yonchuk j. Bioorg Med Chem. 2019 Feb 15;27(4):579-588. doi: 10.1016/j.bmc.2018.12.026. Epub 2018 Dec 21. Bioorg Med Chem. 2019. PMID: 30626555
Characterization of the Potent, Selective Nrf2 Activator, 3-(Pyridin-3-Ylsulfonyl)-5-(Trifluoromethyl)-2H-Chromen-2-One, in Cellular and In Vivo Models of Pulmonary Oxidative Stress.
Yonchuk JG, Foley JP, Bolognese BJ, Logan G, Wixted WE, Kou JP, Chalupowicz DG, Feldser HG, Sanchez Y, Nie H, Callahan JF, Kerns JK, Podolin PL. Yonchuk JG, et al. J Pharmacol Exp Ther. 2017 Oct;363(1):114-125. doi: 10.1124/jpet.117.241794. Epub 2017 Aug 8. J Pharmacol Exp Ther. 2017. PMID: 28790194
Danirixin: A Reversible and Selective Antagonist of the CXC Chemokine Receptor 2.
Busch-Petersen J, Carpenter DC, Burman M, Foley J, Hunsberger GE, Kilian DJ, Salmon M, Mayer RJ, Yonchuk JG, Tal-Singer R. Busch-Petersen J, et al. Among authors: yonchuk jg. J Pharmacol Exp Ther. 2017 Aug;362(2):338-346. doi: 10.1124/jpet.117.240705. Epub 2017 Jun 13. J Pharmacol Exp Ther. 2017. PMID: 28611093
Effect of the CXCR2 antagonist danirixin on symptoms and health status in COPD.
Lazaar AL, Miller BE, Tabberer M, Yonchuk J, Leidy N, Ambery C, Bloomer J, Watz H, Tal-Singer R. Lazaar AL, et al. Among authors: yonchuk j. Eur Respir J. 2018 Oct 4;52(4):1801020. doi: 10.1183/13993003.01020-2018. Print 2018 Oct. Eur Respir J. 2018. PMID: 30139779 Free article. Clinical Trial. No abstract available.
Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations.
Bloomer JC, Ambery C, Miller BE, Connolly P, Garden H, Henley N, Hodnett N, Keel S, Kreindler JL, Lloyd RS, Matthews W, Yonchuk J, Lazaar AL. Bloomer JC, et al. Among authors: yonchuk j. Eur J Pharm Biopharm. 2017 Aug;117:224-231. doi: 10.1016/j.ejpb.2017.03.023. Epub 2017 Apr 3. Eur J Pharm Biopharm. 2017. PMID: 28385615 Clinical Trial.
Soluble receptor for advanced glycation end products (sRAGE) as a biomarker of COPD.
Pratte KA, Curtis JL, Kechris K, Couper D, Cho MH, Silverman EK, DeMeo DL, Sciurba FC, Zhang Y, Ortega VE, O'Neal WK, Gillenwater LA, Lynch DA, Hoffman EA, Newell JD Jr, Comellas AP, Castaldi PJ, Miller BE, Pouwels SD, Hacken NHTT, Bischoff R, Klont F, Woodruff PG, Paine R, Barr RG, Hoidal J, Doerschuk CM, Charbonnier JP, Sung R, Locantore N, Yonchuk JG, Jacobson S, Tal-Singer R, Merrill D, Bowler RP. Pratte KA, et al. Among authors: yonchuk jg. Respir Res. 2021 Apr 27;22(1):127. doi: 10.1186/s12931-021-01686-z. Respir Res. 2021. PMID: 33906653 Free PMC article.