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Inhibition of sphingosine 1-phosphate lyase for the treatment of rheumatoid arthritis: discovery of (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime (LX2931) and (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932).
Bagdanoff JT, Donoviel MS, Nouraldeen A, Carlsen M, Jessop TC, Tarver J, Aleem S, Dong L, Zhang H, Boteju L, Hazelwood J, Yan J, Bednarz M, Layek S, Owusu IB, Gopinathan S, Moran L, Lai Z, Kramer J, Kimball SD, Yalamanchili P, Heydorn WE, Frazier KS, Brooks B, Brown P, Wilson A, Sonnenburg WK, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. Among authors: kramer j. J Med Chem. 2010 Dec 23;53(24):8650-62. doi: 10.1021/jm101183p. Epub 2010 Nov 22. J Med Chem. 2010. PMID: 21090716 Clinical Trial.
Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.
Bagdanoff JT, Donoviel MS, Nouraldeen A, Tarver J, Fu Q, Carlsen M, Jessop TC, Zhang H, Hazelwood J, Nguyen H, Baugh SD, Gardyan M, Terranova KM, Barbosa J, Yan J, Bednarz M, Layek S, Courtney LF, Taylor J, Digeorge-Foushee AM, Gopinathan S, Bruce D, Smith T, Moran L, O'Neill E, Kramer J, Lai Z, Kimball SD, Liu Q, Sun W, Yu S, Swaffield J, Wilson A, Main A, Carson KG, Oravecz T, Augeri DJ. Bagdanoff JT, et al. Among authors: kramer j. J Med Chem. 2009 Jul 9;52(13):3941-53. doi: 10.1021/jm900278w. J Med Chem. 2009. PMID: 19489538
Early toxicology signal generation in the mouse.
Kramer JA, O'Neill E, Phillips ME, Bruce D, Smith T, Albright MM, Bellum S, Gopinathan S, Heydorn WE, Liu X, Nouraldeen A, Payne BJ, Read R, Vogel P, Yu XQ, Wilson AG. Kramer JA, et al. Toxicol Pathol. 2010 Apr;38(3):452-71. doi: 10.1177/0192623310364025. Epub 2010 Mar 19. Toxicol Pathol. 2010. PMID: 20305093
In vivo toxicology of excipients commonly employed in drug discovery in rats.
Gopinathan S, O'Neill E, Rodriguez LA, Champ R, Phillips M, Nouraldeen A, Wendt M, Wilson AGE, Kramer JA. Gopinathan S, et al. J Pharmacol Toxicol Methods. 2013 Sep-Oct;68(2):284-295. doi: 10.1016/j.vascn.2013.02.009. Epub 2013 Mar 14. J Pharmacol Toxicol Methods. 2013. PMID: 23499653
3,405 results