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31 results

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Page 1
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: eksterowicz j. 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: eksterowicz j. 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: eksterowicz j. J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27. J Med Chem. 2014. PMID: 24601644
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC. Li Z, et al. Among authors: eksterowicz j. J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24641103
Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2-p53 Interaction.
Yu M, Wang Y, Zhu J, Bartberger MD, Canon J, Chen A, Chow D, Eksterowicz J, Fox B, Fu J, Gribble M, Huang X, Li Z, Liu JJ, Lo MC, McMinn D, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D. Yu M, et al. Among authors: eksterowicz j. ACS Med Chem Lett. 2014 Jun 30;5(8):894-9. doi: 10.1021/ml500142b. eCollection 2014 Aug 14. ACS Med Chem Lett. 2014. PMID: 25147610 Free PMC article.
Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.
Rew Y, Sun D, Yan X, Beck HP, Canon J, Chen A, Duquette J, Eksterowicz J, Fox BM, Fu J, Gonzalez AZ, Houze J, Huang X, Jiang M, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Saiki AY, Shaffer P, Wang YC, Wortman S, Yakowec P, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Rew Y, et al. Among authors: eksterowicz j. J Med Chem. 2014 Dec 26;57(24):10499-511. doi: 10.1021/jm501550p. Epub 2014 Dec 4. J Med Chem. 2014. PMID: 25384157
Discovery of a Potent Steroidal Glucocorticoid Receptor Antagonist with Enhanced Selectivity against the Progesterone and Androgen Receptors (OP-3633).
Du X, Eksterowicz J, Zhou H, Rew Y, Zhu L, Yan X, Medina JC, Huang T, Chen X, Sutimantanapi D, Jahchan N, Kong W, Sun J, Zavorotinskaya T, Ye Q, Fantin VR, Sun D. Du X, et al. Among authors: eksterowicz j. J Med Chem. 2019 Jul 25;62(14):6751-6764. doi: 10.1021/acs.jmedchem.9b00711. Epub 2019 Jul 5. J Med Chem. 2019. PMID: 31274313
Discovery of a Potent and Selective Steroidal Glucocorticoid Receptor Antagonist (ORIC-101).
Rew Y, Du X, Eksterowicz J, Zhou H, Jahchan N, Zhu L, Yan X, Kawai H, McGee LR, Medina JC, Huang T, Chen C, Zavorotinskaya T, Sutimantanapi D, Waszczuk J, Jackson E, Huang E, Ye Q, Fantin VR, Sun D. Rew Y, et al. Among authors: eksterowicz j. J Med Chem. 2018 Sep 13;61(17):7767-7784. doi: 10.1021/acs.jmedchem.8b00743. Epub 2018 Aug 23. J Med Chem. 2018. PMID: 30091920
Inhibiting NF-κB-inducing kinase (NIK): discovery, structure-based design, synthesis, structure-activity relationship, and co-crystal structures.
Li K, McGee LR, Fisher B, Sudom A, Liu J, Rubenstein SM, Anwer MK, Cushing TD, Shin Y, Ayres M, Lee F, Eksterowicz J, Faulder P, Waszkowycz B, Plotnikova O, Farrelly E, Xiao SH, Chen G, Wang Z. Li K, et al. Among authors: eksterowicz j. Bioorg Med Chem Lett. 2013 Mar 1;23(5):1238-44. doi: 10.1016/j.bmcl.2013.01.012. Epub 2013 Jan 11. Bioorg Med Chem Lett. 2013. PMID: 23374866
31 results