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Page 1
Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement.
Barton LS, Callahan JF, Cantizani J, Concha NO, Cotillo Torrejon I, Goodwin NC, Joshi-Pangu A, Kiesow TJ, McAtee JJ, Mellinger M, Nixon CJ, Padrón-Barthe L, Patterson JR, Pearson ND, Pouliot JJ, Rendina AR, Buitrago Santanilla A, Schneck JL, Sanz O, Thalji RK, Ward P, Williams SP, King BW. Barton LS, et al. Among authors: callahan jf. Bioorg Med Chem. 2024 Feb 15;100:117618. doi: 10.1016/j.bmc.2024.117618. Epub 2024 Jan 29. Bioorg Med Chem. 2024. PMID: 38309201
NRF2 Activation Reprograms Defects in Oxidative Metabolism to Restore Macrophage Function in Chronic Obstructive Pulmonary Disease.
Ryan EM, Sadiku P, Coelho P, Watts ER, Zhang A, Howden AJM, Sanchez-Garcia MA, Bewley M, Cole J, McHugh BJ, Vermaelen W, Ghesquiere B, Carmeliet P, Rodriguez Blanco G, Von Kriegsheim A, Sanchez Y, Rumsey W, Callahan JF, Cooper G, Parkinson N, Baillie K, Cantrell DA, McCafferty J, Choudhury G, Singh D, Dockrell DH, Whyte MKB, Walmsley SR. Ryan EM, et al. Among authors: callahan jf. Am J Respir Crit Care Med. 2023 Apr 15;207(8):998-1011. doi: 10.1164/rccm.202203-0482OC. Am J Respir Crit Care Med. 2023. PMID: 36724365 Free PMC article.
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
Norton D, Bonnette WG, Callahan JF, Carr MG, Griffiths-Jones CM, Heightman TD, Kerns JK, Nie H, Rich SJ, Richardson C, Rumsey W, Sanchez Y, Verdonk ML, Willems HMG, Wixted WE, Wolfe L 3rd, Woolford AJ, Wu Z, Davies TG. Norton D, et al. Among authors: callahan jf. J Med Chem. 2021 Nov 11;64(21):15949-15972. doi: 10.1021/acs.jmedchem.1c01351. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34705450
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Heightman TD, Callahan JF, Chiarparin E, Coyle JE, Griffiths-Jones C, Lakdawala AS, McMenamin R, Mortenson PN, Norton D, Peakman TM, Rich SJ, Richardson C, Rumsey WL, Sanchez Y, Saxty G, Willems HMG, Wolfe L 3rd, Woolford AJ, Wu Z, Yan H, Kerns JK, Davies TG. Heightman TD, et al. Among authors: callahan jf. J Med Chem. 2019 May 9;62(9):4683-4702. doi: 10.1021/acs.jmedchem.9b00279. Epub 2019 Apr 25. J Med Chem. 2019. PMID: 30973731
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: callahan jf. 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. Among authors: callahan jf. 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
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: callahan jf. 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
49 results