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Page 1
Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation.
Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. Podolin PL, et al. Among authors: mellor gw. J Pharmacol Exp Ther. 2005 Jan;312(1):373-81. doi: 10.1124/jpet.104.074484. Epub 2004 Aug 17. J Pharmacol Exp Ther. 2005. PMID: 15316093
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta).
Christopher JA, Bamborough P, Alder C, Campbell A, Cutler GJ, Down K, Hamadi AM, Jolly AM, Kerns JK, Lucas FS, Mellor GW, Miller DD, Morse MA, Pancholi KD, Rumsey W, Solanke YE, Williamson R. Christopher JA, et al. Among authors: mellor gw. J Med Chem. 2009 May 14;52(9):3098-102. doi: 10.1021/jm9000117. J Med Chem. 2009. PMID: 19348415
The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases.
Christopher JA, Avitabile BG, Bamborough P, Champigny AC, Cutler GJ, Dyos SL, Grace KG, Kerns JK, Kitson JD, Mellor GW, Morey JV, Morse MA, O'Malley CF, Patel CB, Probst N, Rumsey W, Smith CA, Wilson MJ. Christopher JA, et al. Among authors: mellor gw. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3972-7. doi: 10.1016/j.bmcl.2007.04.088. Epub 2007 Apr 29. Bioorg Med Chem Lett. 2007. PMID: 17502144
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-β.
Miller DD, Bamborough P, Christopher JA, Baldwin IR, Champigny AC, Cutler GJ, Kerns JK, Longstaff T, Mellor GW, Morey JV, Morse MA, Nie H, Rumsey WL, Taggart JJ. Miller DD, et al. Among authors: mellor gw. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2255-8. doi: 10.1016/j.bmcl.2011.02.107. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21429745
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Liddle J, Bamborough P, Barker MD, Campos S, Cousins RP, Cutler GJ, Hobbs H, Holmes DS, Ioannou C, Mellor GW, Morse MA, Payne JJ, Pritchard JM, Smith KJ, Tape DT, Whitworth C, Williamson RA. Liddle J, et al. Among authors: mellor gw. Bioorg Med Chem Lett. 2009 May 1;19(9):2504-8. doi: 10.1016/j.bmcl.2009.03.034. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19349179
Selectivity of kinase inhibitor fragments.
Bamborough P, Brown MJ, Christopher JA, Chung CW, Mellor GW. Bamborough P, et al. Among authors: mellor gw. J Med Chem. 2011 Jul 28;54(14):5131-43. doi: 10.1021/jm200349b. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21699136
29 results