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Page 1
Cytochrome P450-mediated epoxidation of 2-aminothiazole-based AKT inhibitors: identification of novel GSH adducts and reduction of metabolic activation through structural changes guided by in silico and in vitro screening.
Subramanian R, Lee MR, Allen JG, Bourbeau MP, Fotsch C, Hong FT, Tadesse S, Yao G, Yuan CC, Surapaneni S, Skiles GL, Wang X, Wohlhieter GE, Zeng Q, Zhou Y, Zhu X, Li C. Subramanian R, et al. Among authors: bourbeau mp. Chem Res Toxicol. 2010 Mar 15;23(3):653-63. doi: 10.1021/tx900414g. Chem Res Toxicol. 2010. PMID: 20095585
Azole-based inhibitors of AKT/PKB for the treatment of cancer.
Zeng Q, Allen JG, Bourbeau MP, Wang X, Yao G, Tadesse S, Rider JT, Yuan CC, Hong FT, Lee MR, Zhang S, Lofgren JA, Freeman DJ, Yang S, Li C, Tominey E, Huang X, Hoffman D, Yamane HK, Fotsch C, Dominguez C, Hungate R, Zhang X. Zeng Q, et al. Among authors: bourbeau mp. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1559-64. doi: 10.1016/j.bmcl.2010.01.067. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137943
2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics.
Zeng Q, Bourbeau MP, Wohlhieter GE, Yao G, Monenschein H, Rider JT, Lee MR, Zhang S, Lofgren J, Freeman D, Li C, Tominey E, Huang X, Hoffman D, Yamane H, Tasker AS, Dominguez C, Viswanadhan VN, Hungate R, Zhang X. Zeng Q, et al. Among authors: bourbeau mp. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1652-6. doi: 10.1016/j.bmcl.2010.01.046. Epub 2010 Jan 20. Bioorg Med Chem Lett. 2010. PMID: 20137932
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Pennington LD, et al. Among authors: bourbeau mp. J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1. J Med Chem. 2015. PMID: 26551034 Free article.
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
Allen JG, Bourbeau MP, Wohlhieter GE, Bartberger MD, Michelsen K, Hungate R, Gadwood RC, Gaston RD, Evans B, Mann LW, Matison ME, Schneider S, Huang X, Yu D, Andrews PS, Reichelt A, Long AM, Yakowec P, Yang EY, Lee TA, Oliner JD. Allen JG, et al. Among authors: bourbeau mp. J Med Chem. 2009 Nov 26;52(22):7044-53. doi: 10.1021/jm900681h. J Med Chem. 2009. PMID: 19856920
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase.
Bourbeau MP, Siegmund A, Allen JG, Shu H, Fotsch C, Bartberger MD, Kim KW, Komorowski R, Graham M, Busby J, Wang M, Meyer J, Xu Y, Salyers K, Fielden M, Véniant MM, Gu W. Bourbeau MP, et al. J Med Chem. 2013 Dec 27;56(24):10132-41. doi: 10.1021/jm401601s. Epub 2013 Dec 11. J Med Chem. 2013. PMID: 24294923
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.
Harrington PE, Bourbeau MP, Fotsch C, Frohn M, Pickrell AJ, Reichelt A, Sham K, Siegmund AC, Bailis JM, Bush T, Escobar S, Hickman D, Heller S, Hsieh F, Orf JN, Rong M, San Miguel T, Tan H, Zalameda L, Allen JG. Harrington PE, et al. Among authors: bourbeau mp. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6396-400. doi: 10.1016/j.bmcl.2013.09.055. Epub 2013 Sep 25. Bioorg Med Chem Lett. 2013. PMID: 24120542
Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).
Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR. Hu E, et al. Among authors: bourbeau mp. J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4. J Med Chem. 2014. PMID: 25062128
Nonracemic synthesis of GK-GKRP disruptor AMG-3969.
Bourbeau MP, Ashton KS, Yan J, St Jean DJ Jr. Bourbeau MP, et al. J Org Chem. 2014 Apr 18;79(8):3684-7. doi: 10.1021/jo500336e. Epub 2014 Apr 10. J Org Chem. 2014. PMID: 24678849
20 results