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Discovery of CC-99677, a selective targeted covalent MAPKAPK2 (MK2) inhibitor for autoimmune disorders.
Malona J, Chuaqui C, Seletsky BM, Beebe L, Cantin S, Kalken DV, Fahnoe K, Wang Z, Browning B, Szabo H, Koopman LA, Oravecz T, McDonald JJ, Ramirez-Valle F, Gaur R, Mensah KA, Thomas M, Connarn JN, Hu H, Alexander MD, Corin AF. Malona J, et al. Among authors: oravecz t. Transl Res. 2022 Nov;249:49-73. doi: 10.1016/j.trsl.2022.06.005. Epub 2022 Jun 9. Transl Res. 2022. PMID: 35691544 Free article.
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: oravecz t. J Med Chem. 2009 Jul 9;52(13):3941-53. doi: 10.1021/jm900278w. J Med Chem. 2009. PMID: 19489538
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: oravecz t. 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.
5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase.
Tarver JE, Jessop TC, Carlsen M, Augeri DJ, Fu Q, Healy JP, Heim-Riether A, Xu A, Taylor JA, Shen M, Keyes PE, David Kimball S, Yu XC, Miranda M, Liu Q, Swaffield JC, Nouraldeen A, Wilson AG, Finch R, Jhaver K, Foushee AM, Anderson S, Oravecz T, Carson KG. Tarver JE, et al. Among authors: oravecz t. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6780-3. doi: 10.1016/j.bmcl.2009.09.082. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19836229
Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.
Jessop TC, Tarver JE, Carlsen M, Xu A, Healy JP, Heim-Riether A, Fu Q, Taylor JA, Augeri DJ, Shen M, Stouch TR, Swanson RV, Tari LW, Hunter M, Hoffman I, Keyes PE, Yu XC, Miranda M, Liu Q, Swaffield JC, David Kimball S, Nouraldeen A, Wilson AG, Foushee AM, Jhaver K, Finch R, Anderson S, Oravecz T, Carson KG. Jessop TC, et al. Among authors: oravecz t. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6784-7. doi: 10.1016/j.bmcl.2009.09.081. Epub 2009 Sep 25. Bioorg Med Chem Lett. 2009. PMID: 19836232
Genetic deletion of Mst1 alters T cell function and protects against autoimmunity.
Salojin KV, Hamman BD, Chang WC, Jhaver KG, Al-Shami A, Crisostomo J, Wilkins C, Digeorge-Foushee AM, Allen J, Patel N, Gopinathan S, Zhou J, Nouraldeen A, Jessop TC, Bagdanoff JT, Augeri DJ, Read R, Vogel P, Swaffield J, Wilson A, Platt KA, Carson KG, Main A, Zambrowicz BP, Oravecz T. Salojin KV, et al. Among authors: oravecz t. PLoS One. 2014 May 22;9(5):e98151. doi: 10.1371/journal.pone.0098151. eCollection 2014. PLoS One. 2014. PMID: 24852423 Free PMC article.
50 results