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Page 1
Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.
Heald RA, Jackson P, Savy P, Jones M, Gancia E, Burton B, Newman R, Boggs J, Chan E, Chan J, Choo E, Merchant M, Rudewicz P, Ultsch M, Wiesmann C, Yue Q, Belvin M, Price S. Heald RA, et al. Among authors: burton b. J Med Chem. 2012 May 24;55(10):4594-604. doi: 10.1021/jm2017094. Epub 2012 May 3. J Med Chem. 2012. PMID: 22506516
Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P, Burton B, Choo EF, Pang J, Boggs J, Yang A, Yang X, Baumgardner M. Robarge KD, et al. Among authors: burton b. Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723. doi: 10.1016/j.bmcl.2014.08.008. Epub 2014 Aug 15. Bioorg Med Chem Lett. 2014. PMID: 25193232
Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
Gazzard L, Williams K, Chen H, Axford L, Blackwood E, Burton B, Chapman K, Crackett P, Drobnick J, Ellwood C, Epler J, Flagella M, Gancia E, Gill M, Goodacre S, Halladay J, Hewitt J, Hunt H, Kintz S, Lyssikatos J, Macleod C, Major S, Médard G, Narukulla R, Ramiscal J, Schmidt S, Seward E, Wiesmann C, Wu P, Yee S, Yen I, Malek S. Gazzard L, et al. Among authors: burton b. J Med Chem. 2015 Jun 25;58(12):5053-74. doi: 10.1021/acs.jmedchem.5b00464. Epub 2015 Jun 4. J Med Chem. 2015. PMID: 25988399
Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.
Fauber BP, Gobbi A, Savy P, Burton B, Deng Y, Everett C, La H, Johnson AR, Lockey P, Norman M, Wong H. Fauber BP, et al. Among authors: burton b. Bioorg Med Chem Lett. 2015 Oct 1;25(19):4109-13. doi: 10.1016/j.bmcl.2015.08.028. Epub 2015 Aug 14. Bioorg Med Chem Lett. 2015. PMID: 26321361
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
Morley AD, Kenny PW, Burton B, Heald RA, Macfaul PA, Mullett J, Page K, Porres SS, Ribeiro LR, Smith P, Ward S, Wilkinson TJ. Morley AD, et al. Among authors: burton b. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1658-61. doi: 10.1016/j.bmcl.2009.01.110. Epub 2009 Feb 6. Bioorg Med Chem Lett. 2009. PMID: 19231183
Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.
Fauber BP, René O, de Leon Boenig G, Burton B, Deng Y, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, La H, Liimatta M, Lockey P, Norman M, Ouyang W, Wang W, Wong H. Fauber BP, et al. Among authors: burton b. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3891-7. doi: 10.1016/j.bmcl.2014.06.048. Epub 2014 Jun 25. Bioorg Med Chem Lett. 2014. PMID: 25017032
Identification of tertiary sulfonamides as RORc inverse agonists.
Fauber BP, René O, Burton B, Everett C, Gobbi A, Hawkins J, Johnson AR, Liimatta M, Lockey P, Norman M, Wong H. Fauber BP, et al. Among authors: burton b. Bioorg Med Chem Lett. 2014 May 1;24(9):2182-7. doi: 10.1016/j.bmcl.2014.03.038. Epub 2014 Mar 21. Bioorg Med Chem Lett. 2014. PMID: 24685544
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
René O, Fauber BP, Boenig Gde L, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Kiefer JR, Liimatta M, Lockey P, Norman M, Ouyang W, Wallweber HA, Wong H. René O, et al. Among authors: burton b. ACS Med Chem Lett. 2014 Dec 4;6(3):276-81. doi: 10.1021/ml500420y. eCollection 2015 Mar 12. ACS Med Chem Lett. 2014. PMID: 25815138 Free PMC article.
797 results