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Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, Mutnick D, Bursulaya B, Schmeits J, Wu X, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Seidel HM, Molteni V, Liu B, Phimister A, Joseph SB, Laffitte B. Tully DC, et al. Among authors: bursulaya b. J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29148806
Identification of novel potent bicyclic peptide deformylase inhibitors.
Molteni V, He X, Nabakka J, Yang K, Kreusch A, Gordon P, Bursulaya B, Warner I, Shin T, Biorac T, Ryder NS, Goldberg R, Doughty J, He Y. Molteni V, et al. Among authors: bursulaya b. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1477-81. doi: 10.1016/j.bmcl.2004.01.014. Bioorg Med Chem Lett. 2004. PMID: 15006385
1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
Epple R, Azimioara M, Russo R, Bursulaya B, Tian SS, Gerken A, Iskandar M. Epple R, et al. Among authors: bursulaya b. Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. doi: 10.1016/j.bmcl.2006.02.079. Epub 2006 Mar 20. Bioorg Med Chem Lett. 2006. PMID: 16546385
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Epple R, Azimioara M, Russo R, Xie Y, Wang X, Cow C, Wityak J, Karanewsky D, Bursulaya B, Kreusch A, Tuntland T, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS. Epple R, et al. Among authors: bursulaya b. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5488-92. doi: 10.1016/j.bmcl.2006.08.052. Epub 2006 Aug 22. Bioorg Med Chem Lett. 2006. PMID: 16931011
Discovery of inhibitors of the channel-activating protease prostasin (CAP1/PRSS8) utilizing structure-based design.
Tully DC, Vidal A, Chatterjee AK, Williams JA, Roberts MJ, Petrassi HM, Spraggon G, Bursulaya B, Pacoma R, Shipway A, Schumacher AM, Danahay H, Harris JL. Tully DC, et al. Among authors: bursulaya b. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5895-9. doi: 10.1016/j.bmcl.2008.08.029. Epub 2008 Aug 14. Bioorg Med Chem Lett. 2008. PMID: 18752942
Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.
Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. Marsilje TH, et al. Among authors: bursulaya b. J Med Chem. 2013 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26. J Med Chem. 2013. PMID: 23742252
49 results