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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: yan h. 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: yan h. 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
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: yan h. 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
Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.
Lainé DI, Yan H, Xie H, Davis RS, Dufour J, Widdowson KL, Palovich MR, Wan Z, Foley JJ, Schmidt DB, Hunsberger GE, Burman M, Bacon AM, Webb EF, Luttmann MA, Salmon M, Sarau HM, Umbrecht ST, Landis PS, Peck BJ, Busch-Petersen J. Lainé DI, et al. Among authors: yan h. Bioorg Med Chem Lett. 2012 May 1;22(9):3366-9. doi: 10.1016/j.bmcl.2012.02.015. Epub 2012 Feb 15. Bioorg Med Chem Lett. 2012. PMID: 22460029
Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD.
Wan Z, Laine DI, Yan H, Zhu C, Widdowson KL, Buckley PT, Burman M, Foley JJ, Sarau HM, Schmidt DB, Webb EF, Belmonte KE, Palovich M. Wan Z, et al. Among authors: yan h. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4560-2. doi: 10.1016/j.bmcl.2009.07.006. Epub 2009 Jul 8. Bioorg Med Chem Lett. 2009. PMID: 19616944
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