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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: huang x. J Med Chem. 2009 Nov 26;52(22):7044-53. doi: 10.1021/jm900681h. J Med Chem. 2009. PMID: 19856920
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: huang x. 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
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: huang x. 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
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
Rew Y, Sun D, Gonzalez-Lopez De Turiso F, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Deignan J, Fox BM, Gustin D, Huang X, Jiang M, Jiao X, Jin L, Kayser F, Kopecky DJ, Li Y, Lo MC, Long AM, Michelsen K, Oliner JD, Osgood T, Ragains M, Saiki AY, Schneider S, Toteva M, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Rew Y, et al. Among authors: huang x. J Med Chem. 2012 Jun 14;55(11):4936-54. doi: 10.1021/jm300354j. Epub 2012 May 9. J Med Chem. 2012. PMID: 22524527
Rational design and binding mode duality of MDM2-p53 inhibitors.
Gonzalez-Lopez de Turiso F, Sun D, Rew Y, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Correll TL, Huang X, Julian LD, Kayser F, Lo MC, Long AM, McMinn D, Oliner JD, Osgood T, Powers JP, Saiki AY, Schneider S, Shaffer P, Xiao SH, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Gonzalez-Lopez de Turiso F, et al. Among authors: huang x. J Med Chem. 2013 May 23;56(10):4053-70. doi: 10.1021/jm400293z. Epub 2013 May 6. J Med Chem. 2013. PMID: 23597064
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC. Sun D, et al. Among authors: huang x. J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24456472
Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.
Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D. Gonzalez AZ, et al. Among authors: huang x. J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4. J Med Chem. 2014. PMID: 24548297
Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.
Gonzalez AZ, Li Z, Beck HP, Canon J, Chen A, Chow D, Duquette J, Eksterowicz J, Fox BM, Fu J, Huang X, Houze J, Jin L, Li Y, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Sun D, Medina JC. Gonzalez AZ, et al. Among authors: huang x. J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27. J Med Chem. 2014. PMID: 24601644
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