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Page 1
Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.
Goedken ER, Argiriadi MA, Banach DL, Fiamengo BA, Foley SE, Frank KE, George JS, Harris CM, Hobson AD, Ihle DC, Marcotte D, Merta PJ, Michalak ME, Murdock SE, Tomlinson MJ, Voss JW. Goedken ER, et al. Among authors: george js. J Biol Chem. 2015 Feb 20;290(8):4573-4589. doi: 10.1074/jbc.M114.595181. Epub 2014 Dec 31. J Biol Chem. 2015. PMID: 25552479 Free PMC article.
Structure activity optimization of 6H-pyrrolo[2,3-e][1,2,4]triazolo[4,3-a]pyrazines as Jak1 kinase inhibitors.
Friedman M, Frank KE, Aguirre A, Argiriadi MA, Davis H, Edmunds JJ, George DM, George JS, Goedken E, Fiamengo B, Hyland D, Li B, Murtaza A, Morytko M, Somal G, Stewart K, Tarcsa E, Van Epps S, Voss J, Wang L, Woller K, Wishart N. Friedman M, et al. Among authors: george dm, george js. Bioorg Med Chem Lett. 2015 Oct 15;25(20):4399-404. doi: 10.1016/j.bmcl.2015.09.020. Epub 2015 Sep 8. Bioorg Med Chem Lett. 2015. PMID: 26372653
Design and synthesis of tricyclic cores for kinase inhibition.
Van Epps S, Fiamengo B, Edmunds J, Ericsson A, Frank K, Friedman M, George D, George J, Goedken E, Kotecki B, Martinez G, Merta P, Morytko M, Shekhar S, Skinner B, Stewart K, Voss J, Wallace G, Wang L, Wang L, Wishart N. Van Epps S, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):693-8. doi: 10.1016/j.bmcl.2012.11.108. Epub 2012 Dec 5. Bioorg Med Chem Lett. 2013. PMID: 23265875
In vitro and in vivo characterization of the JAK1 selectivity of upadacitinib (ABT-494).
Parmentier JM, Voss J, Graff C, Schwartz A, Argiriadi M, Friedman M, Camp HS, Padley RJ, George JS, Hyland D, Rosebraugh M, Wishart N, Olson L, Long AJ. Parmentier JM, et al. Among authors: george js. BMC Rheumatol. 2018 Aug 28;2:23. doi: 10.1186/s41927-018-0031-x. eCollection 2018. BMC Rheumatol. 2018. PMID: 30886973 Free PMC article.
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Betschmann P, Bettencourt B, Donnelly-Roberts D, Friedman M, George J, Hirst G, Josephsohn N, Konopacki D, Li B, Maull J, Morytko MJ, Moore NS, Namovic M, Rafferty P, Salmeron-Garcia JA, Tarcsa E, Wang L, Woller K. Betschmann P, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):3848-51. doi: 10.1016/j.bmcl.2008.06.055. Epub 2008 Jun 20. Bioorg Med Chem Lett. 2008. PMID: 18595695
104 results