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Items: 30

1.

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.

J Med Chem. 2019 Jul 25;62(14):6751-6764. doi: 10.1021/acs.jmedchem.9b00711. Epub 2019 Jul 5.

PMID:
31274313
2.

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.

J Med Chem. 2018 Sep 13;61(17):7767-7784. doi: 10.1021/acs.jmedchem.8b00743. Epub 2018 Aug 23.

PMID:
30091920
3.

Structural and Functional Characterization of the JH2 Pseudokinase Domain of JAK Family Tyrosine Kinase 2 (TYK2).

Min X, Ungureanu D, Maxwell S, Hammarén H, Thibault S, Hillert EK, Ayres M, Greenfield B, Eksterowicz J, Gabel C, Walker N, Silvennoinen O, Wang Z.

J Biol Chem. 2015 Nov 6;290(45):27261-70. doi: 10.1074/jbc.M115.672048. Epub 2015 Sep 10.

4.

The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents.

Canon J, Osgood T, Olson SH, Saiki AY, Robertson R, Yu D, Eksterowicz J, Ye Q, Jin L, Chen A, Zhou J, Cordover D, Kaufman S, Kendall R, Oliner JD, Coxon A, Radinsky R.

Mol Cancer Ther. 2015 Mar;14(3):649-58. doi: 10.1158/1535-7163.MCT-14-0710. Epub 2015 Jan 7.

5.

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.

J Med Chem. 2014 Dec 26;57(24):10499-511. doi: 10.1021/jm501550p. Epub 2014 Dec 4.

PMID:
25384157
6.

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.

ACS Med Chem Lett. 2014 Jun 30;5(8):894-9. doi: 10.1021/ml500142b. eCollection 2014 Aug 14.

7.

Characterization of the active site properties of CYP4F12.

Eksterowicz J, Rock DA, Rock BM, Wienkers LC, Foti RS.

Drug Metab Dispos. 2014 Oct;42(10):1698-707. doi: 10.1124/dmd.114.059626. Epub 2014 Jul 29.

PMID:
25074871
8.

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.

J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2.

PMID:
24641103
9.

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.

J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27.

PMID:
24601644
10.

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.

J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4.

PMID:
24548297
11.

Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia.

Keegan K, Li C, Li Z, Ma J, Ragains M, Coberly S, Hollenback D, Eksterowicz J, Liang L, Weidner M, Huard J, Wang X, Alba G, Orf J, Lo MC, Zhao S, Ngo R, Chen A, Liu L, Carlson T, Quéva C, McGee LR, Medina J, Kamb A, Wickramasinghe D, Dai K.

Mol Cancer Ther. 2014 Apr;13(4):880-9. doi: 10.1158/1535-7163.MCT-13-0858. Epub 2014 Feb 13.

12.

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.

J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5.

PMID:
24456472
13.

Discovery and optimization of arylsulfonyl 3-(pyridin-2-yloxy)anilines as novel GPR119 agonists.

Zhang JK, Li AR, Yu M, Wang Y, Zhu J, Kayser F, Medina JC, Siegler K, Conn M, Shan B, Grillo MP, Eksterowicz J, Coward P, Liu JJ.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3609-13. doi: 10.1016/j.bmcl.2013.04.014. Epub 2013 Apr 15.

PMID:
23648181
14.

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.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1238-44. doi: 10.1016/j.bmcl.2013.01.012. Epub 2013 Jan 11.

PMID:
23374866
15.

Development of a time-resolved fluorescence resonance energy transfer assay for cyclin-dependent kinase 4 and identification of its ATP-noncompetitive inhibitors.

Lo MC, Ngo R, Dai K, Li C, Liang L, Lee J, Emkey R, Eksterowicz J, Ventura M, Young SW, Xiao SH.

Anal Biochem. 2012 Feb 15;421(2):368-77. doi: 10.1016/j.ab.2011.10.014. Epub 2011 Oct 12.

PMID:
22056947
16.

Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.

Cheng AC, Eksterowicz J, Geuns-Meyer S, Sun Y.

J Med Chem. 2010 Jun 10;53(11):4502-10. doi: 10.1021/jm100301x.

PMID:
20459125
18.

Facile synthesis of substituted 5-amino- and 3-amino-1,2,4-thiadiazoles from a common precursor.

Wehn PM, Harrington PE, Eksterowicz JE.

Org Lett. 2009 Dec 17;11(24):5666-9. doi: 10.1021/ol902371y.

PMID:
20000443
19.

Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.

Moree WJ, Goldman P, Demaggio AJ, Christenson E, Herendeen D, Eksterowicz J, Kesicki EA, McElligott DL, Beaton G.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5126-9. doi: 10.1016/j.bmcl.2008.07.091. Epub 2008 Jul 27.

PMID:
18713665
20.

[Evaluation of the way of nutrition of the physical education students during summer sports camp].

Eksterowicz J, Napierała M.

Rocz Panstw Zakl Hig. 2008;59(1):75-82. Polish.

21.

Significance analysis and multiple pharmacophore models for differentiating P-glycoprotein substrates.

Li WX, Li L, Eksterowicz J, Ling XB, Cardozo M.

J Chem Inf Model. 2007 Nov-Dec;47(6):2429-38. Epub 2007 Oct 23.

PMID:
17956085
22.

Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo.

Spencer JR, Sendzik M, Oeh J, Sabbatini P, Dalrymple SA, Magill C, Kim HM, Zhang P, Squires N, Moss KG, Sukbuntherng J, Graupe D, Eksterowicz J, Young PR, Myers AG, Green MJ.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4884-8. Epub 2006 Jul 25.

PMID:
16870445
23.

Discovery and structure-activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers.

Tai VW, Sperandio D, Shelton EJ, Litvak J, Pararajasingham K, Cebon B, Lohman J, Eksterowicz J, Kantak S, Sabbatini P, Brown C, Zeitz J, Reed C, Maske B, Graupe D, Estevez A, Oeh J, Wong D, Ni Y, Sprengeler P, Yee R, Magill C, Neri A, Cai SX, Drewe J, Qiu L, Herich J, Tseng B, Kasibhatla S, Spencer JR.

Bioorg Med Chem Lett. 2006 Sep 1;16(17):4554-8. Epub 2006 Jun 19.

PMID:
16784854
24.

Performance of 3D-database molecular docking studies into homology models.

Oshiro C, Bradley EK, Eksterowicz J, Evensen E, Lamb ML, Lanctot JK, Putta S, Stanton R, Grootenhuis PD.

J Med Chem. 2004 Jan 29;47(3):764-7.

PMID:
14736258
25.

Comparing performance of computational tools for combinatorial library design.

Evensen E, Eksterowicz JE, Stanton RV, Oshiro C, Grootenhuis PD, Bradley EK.

J Med Chem. 2003 Nov 20;46(24):5125-8.

PMID:
14613315
26.

A novel subshape molecular descriptor.

Putta S, Eksterowicz J, Lemmen C, Stanton R.

J Chem Inf Comput Sci. 2003 Sep-Oct;43(5):1623-35.

PMID:
14502497
27.

Coupling structure-based design with combinatorial chemistry: application of active site derived pharmacophores with informative library design.

Eksterowicz JE, Evensen E, Lemmen C, Brady GP, Lanctot JK, Bradley EK, Saiah E, Robinson LA, Grootenhuis PD, Blaney JM.

J Mol Graph Model. 2002 Jun;20(6):469-77.

PMID:
12071281
28.

Evaluation of a novel shape-based computational filter for lead evolution: application to thrombin inhibitors.

Srinivasan J, Castellino A, Bradley EK, Eksterowicz JE, Grootenhuis PD, Putta S, Stanton RV.

J Med Chem. 2002 Jun 6;45(12):2494-500.

PMID:
12036357
29.

Applications of random sampling to virtual screening of combinatorial libraries.

Beroza P, Bradley EK, Eksterowicz JE, Feinstein R, Greene J, Grootenhuis PD, Henne RM, Mount J, Shirley WA, Smellie A, Stanton RV, Spellmeyer DC.

J Mol Graph Model. 2000 Aug-Oct;18(4-5):335-42.

PMID:
11143553

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