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Items: 1 to 50 of 75

1.

Tumor-derived CK1α mutations enhance MDMX inhibition of p53.

Liu X, Huang Q, Chen L, Zhang H, Schonbrunn E, Chen J.

Oncogene. 2019 Aug 28. doi: 10.1038/s41388-019-0979-z. [Epub ahead of print]

PMID:
31462704
2.

Design, Synthesis, and Characterization of a Fluorescence Polarization Pan-BET Bromodomain Probe.

Paulson CN, Guan X, Ayoub AM, Chan A, Karim RM, Pomerantz WCK, Schönbrunn E, Georg GI, Hawkinson JE.

ACS Med Chem Lett. 2018 Oct 31;9(12):1223-1229. doi: 10.1021/acsmedchemlett.8b00380. eCollection 2018 Dec 13.

PMID:
30613330
3.

Molecular Basis for the N-Terminal Bromodomain-and-Extra-Terminal-Family Selectivity of a Dual Kinase-Bromodomain Inhibitor.

Divakaran A, Talluri SK, Ayoub AM, Mishra NK, Cui H, Widen JC, Berndt N, Zhu JY, Carlson AS, Topczewski JJ, Schonbrunn EK, Harki DA, Pomerantz WCK.

J Med Chem. 2018 Oct 25;61(20):9316-9334. doi: 10.1021/acs.jmedchem.8b01248. Epub 2018 Oct 16.

4.

Targeting the BRD4-HOXB13 Coregulated Transcriptional Networks with Bromodomain-Kinase Inhibitors to Suppress Metastatic Castration-Resistant Prostate Cancer.

Nerlakanti N, Yao J, Nguyen DT, Patel AK, Eroshkin AM, Lawrence HR, Ayaz M, Kuenzi BM, Agarwal N, Chen Y, Gunawan S, Karim RM, Berndt N, Puskas J, Magliocco AM, Coppola D, Dhillon J, Zhang J, Shymalagovindarajan S, Rix U, Kim Y, Perera R, Lawrence NJ, Schonbrunn E, Mahajan K.

Mol Cancer Ther. 2018 Dec;17(12):2796-2810. doi: 10.1158/1535-7163.MCT-18-0602. Epub 2018 Sep 21.

PMID:
30242092
5.

Ligand-mediated protein degradation reveals functional conservation among sequence variants of the CUL4-type E3 ligase substrate receptor cereblon.

Akuffo AA, Alontaga AY, Metcalf R, Beatty MS, Becker A, McDaniel JM, Hesterberg RS, Goodheart WE, Gunawan S, Ayaz M, Yang Y, Karim MR, Orobello ME, Daniel K, Guida W, Yoder JA, Rajadhyaksha AM, Schönbrunn E, Lawrence HR, Lawrence NJ, Epling-Burnette PK.

J Biol Chem. 2018 Apr 20;293(16):6187-6200. doi: 10.1074/jbc.M117.816868. Epub 2018 Feb 15.

6.

Structural Basis of ALDH1A2 Inhibition by Irreversible and Reversible Small Molecule Inhibitors.

Chen Y, Zhu JY, Hong KH, Mikles DC, Georg GI, Goldstein AS, Amory JK, Schönbrunn E.

ACS Chem Biol. 2018 Mar 16;13(3):582-590. doi: 10.1021/acschembio.7b00685. Epub 2018 Jan 3.

7.

Structure-Activity Studies of N-Butyl-1-deoxynojirimycin (NB-DNJ) Analogues: Discovery of Potent and Selective Aminocyclopentitol Inhibitors of GBA1 and GBA2.

Gu X, Gupta V, Yang Y, Zhu JY, Carlson EJ, Kingsley C, Tash JS, Schönbrunn E, Hawkinson J, Georg GI.

ChemMedChem. 2017 Dec 7;12(23):1977-1984. doi: 10.1002/cmdc.201700558. Epub 2017 Nov 24.

8.

Identification of a Novel Class of BRD4 Inhibitors by Computational Screening and Binding Simulations.

Allen BK, Mehta S, Ember SWJ, Zhu JY, Schönbrunn E, Ayad NG, Schürer SC.

ACS Omega. 2017 Aug 31;2(8):4760-4771. doi: 10.1021/acsomega.7b00553. Epub 2017 Aug 21.

9.

Structural Basis of Wee Kinases Functionality and Inactivation by Diverse Small Molecule Inhibitors.

Zhu JY, Cuellar RA, Berndt N, Lee HE, Olesen SH, Martin MP, Jensen JT, Georg GI, Schönbrunn E.

J Med Chem. 2017 Sep 28;60(18):7863-7875. doi: 10.1021/acs.jmedchem.7b00996. Epub 2017 Sep 14.

10.

Advances of small molecule targeting of kinases.

Berndt N, Karim RM, Schönbrunn E.

Curr Opin Chem Biol. 2017 Aug;39:126-132. doi: 10.1016/j.cbpa.2017.06.015. Epub 2017 Jul 18. Review.

11.

Correction to BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jul 27;60(14):6458. doi: 10.1021/acs.jmedchem.7b00943. Epub 2017 Jul 11. No abstract available.

PMID:
28696689
12.

Dual Targeting of WEE1 and PLK1 by AZD1775 Elicits Single Agent Cellular Anticancer Activity.

Wright G, Golubeva V, Remsing Rix LL, Berndt N, Luo Y, Ward GA, Gray JE, Schonbrunn E, Lawrence HR, Monteiro ANA, Rix U.

ACS Chem Biol. 2017 Jul 21;12(7):1883-1892. doi: 10.1021/acschembio.7b00147. Epub 2017 Jun 7.

13.

BET Bromodomain Inhibitors with One-Step Synthesis Discovered from Virtual Screen.

Ayoub AM, Hawk LML, Herzig RJ, Jiang J, Wisniewski AJ, Gee CT, Zhao P, Zhu JY, Berndt N, Offei-Addo NK, Scott TG, Qi J, Bradner JE, Ward TR, Schönbrunn E, Georg GI, Pomerantz WCK.

J Med Chem. 2017 Jun 22;60(12):4805-4817. doi: 10.1021/acs.jmedchem.6b01336. Epub 2017 Jun 7. Erratum in: J Med Chem. 2017 Jul 27;60(14):6458.

14.
15.

Potent Dual BET Bromodomain-Kinase Inhibitors as Value-Added Multitargeted Chemical Probes and Cancer Therapeutics.

Ember SW, Lambert QT, Berndt N, Gunawan S, Ayaz M, Tauro M, Zhu JY, Cranfill PJ, Greninger P, Lynch CC, Benes CH, Lawrence HR, Reuther GW, Lawrence NJ, Schönbrunn E.

Mol Cancer Ther. 2017 Jun;16(6):1054-1067. doi: 10.1158/1535-7163.MCT-16-0568-T. Epub 2017 Mar 23.

16.

Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET.

Koblan LW, Buckley DL, Ott CJ, Fitzgerald ME, Ember SW, Zhu JY, Liu S, Roberts JM, Remillard D, Vittori S, Zhang W, Schonbrunn E, Bradner JE.

ChemMedChem. 2016 Dec 6;11(23):2575-2581. doi: 10.1002/cmdc.201600502. Epub 2016 Nov 15.

PMID:
27862999
17.

Discovery of Diverse Small-Molecule Inhibitors of Mammalian Sterile20-like Kinase 3 (MST3).

Olesen SH, Zhu JY, Martin MP, Schönbrunn E.

ChemMedChem. 2016 Jun 6;11(11):1137-44. doi: 10.1002/cmdc.201600115. Epub 2016 May 2.

PMID:
27135311
18.

An Advanced Tool To Interrogate BRD9.

Karim RM, Schönbrunn E.

J Med Chem. 2016 May 26;59(10):4459-61. doi: 10.1021/acs.jmedchem.6b00550. Epub 2016 Apr 27.

PMID:
27120693
19.

Correction to Letter: Fluorinated Aromatic Amino Acids Are Sensitive (19)F NMR Probes for Bromodomain-Ligand Interactions.

Mishra NK, Urick AK, Ember SW, Schönbrunn E, Pomerantz WC.

ACS Chem Biol. 2016 Apr 15;11(4):1149. doi: 10.1021/acschembio.6b00049. Epub 2016 Feb 2. No abstract available.

20.

Large-Scale Computational Screening Identifies First in Class Multitarget Inhibitor of EGFR Kinase and BRD4.

Allen BK, Mehta S, Ember SW, Schonbrunn E, Ayad N, Schürer SC.

Sci Rep. 2015 Nov 24;5:16924. doi: 10.1038/srep16924.

21.

Autoinhibition of MDMX by intramolecular p53 mimicry.

Chen L, Borcherds W, Wu S, Becker A, Schonbrunn E, Daughdrill GW, Chen J.

Proc Natl Acad Sci U S A. 2015 Apr 14;112(15):4624-9. doi: 10.1073/pnas.1420833112. Epub 2015 Mar 30.

22.

Stability of the human Hsp90-p50Cdc37 chaperone complex against nucleotides and Hsp90 inhibitors, and the influence of phosphorylation by casein kinase 2.

Olesen SH, Ingles DJ, Zhu JY, Martin MP, Betzi S, Georg GI, Tash JS, Schönbrunn E.

Molecules. 2015 Jan 19;20(1):1643-60. doi: 10.3390/molecules20011643.

23.

Fluorinated aromatic amino acids are sensitive 19F NMR probes for bromodomain-ligand interactions.

Mishra NK, Urick AK, Ember SW, Schönbrunn E, Pomerantz WC.

ACS Chem Biol. 2014 Dec 19;9(12):2755-60. doi: 10.1021/cb5007344. Epub 2014 Oct 27. Erratum in: ACS Chem Biol. 2016 Apr 15;11(4):1149.

24.

Dual Aurora A and JAK2 kinase blockade effectively suppresses malignant transformation.

Yang H, Lawrence HR, Kazi A, Gevariya H, Patel R, Luo Y, Rix U, Schonbrunn E, Lawrence NJ, Sebti SM.

Oncotarget. 2014 May 30;5(10):2947-61.

25.

Acetyl-lysine binding site of bromodomain-containing protein 4 (BRD4) interacts with diverse kinase inhibitors.

Ember SW, Zhu JY, Olesen SH, Martin MP, Becker A, Berndt N, Georg GI, Schönbrunn E.

ACS Chem Biol. 2014 May 16;9(5):1160-71. doi: 10.1021/cb500072z. Epub 2014 Mar 13.

26.

MurA as a primary target of tulipalin B and 6-tuliposide B.

Shigetomi K, Olesen SH, Yang Y, Mitsuhashi S, Schönbrunn E, Ubukata M.

Biosci Biotechnol Biochem. 2013;77(12):2517-9. Epub 2013 Dec 7.

27.

Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains.

Martin MP, Olesen SH, Georg GI, Schönbrunn E.

ACS Chem Biol. 2013 Nov 15;8(11):2360-5. doi: 10.1021/cb4003283. Epub 2013 Sep 10.

28.

Differential antibacterial properties of the MurA inhibitors terreic acid and fosfomycin.

Olesen SH, Ingles DJ, Yang Y, Schönbrunn E.

J Basic Microbiol. 2014 Apr;54(4):322-6. doi: 10.1002/jobm.201200617. Epub 2013 May 20.

29.

Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.

Schonbrunn E, Betzi S, Alam R, Martin MP, Becker A, Han H, Francis R, Chakrasali R, Jakkaraj S, Kazi A, Sebti SM, Cubitt CL, Gebhard AW, Hazlehurst LA, Tash JS, Georg GI.

J Med Chem. 2013 May 23;56(10):3768-82. doi: 10.1021/jm301234k. Epub 2013 May 6.

30.

Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).

Pireddu R, Forinash KD, Sun NN, Martin MP, Sung SS, Alexander B, Zhu JY, Guida WC, Schönbrunn E, Sebti SM, Lawrence NJ.

Medchemcomm. 2012 Jun 1;3(6):699-709. Epub 2012 Jan 27.

31.

Casein kinase 1α regulates an MDMX intramolecular interaction to stimulate p53 binding.

Wu S, Chen L, Becker A, Schonbrunn E, Chen J.

Mol Cell Biol. 2012 Dec;32(23):4821-32. doi: 10.1128/MCB.00851-12. Epub 2012 Oct 1.

32.

A novel approach to the discovery of small-molecule ligands of CDK2.

Martin MP, Alam R, Betzi S, Ingles DJ, Zhu JY, Schönbrunn E.

Chembiochem. 2012 Sep 24;13(14):2128-36. doi: 10.1002/cbic.201200316. Epub 2012 Aug 14.

33.

RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer.

Patel RA, Forinash KD, Pireddu R, Sun Y, Sun N, Martin MP, Schönbrunn E, Lawrence NJ, Sebti SM.

Cancer Res. 2012 Oct 1;72(19):5025-34. doi: 10.1158/0008-5472.CAN-12-0954. Epub 2012 Jul 30.

34.

Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

Lawrence HR, Martin MP, Luo Y, Pireddu R, Yang H, Gevariya H, Ozcan S, Zhu JY, Kendig R, Rodriguez M, Elias R, Cheng JQ, Sebti SM, Schonbrunn E, Lawrence NJ.

J Med Chem. 2012 Sep 13;55(17):7392-7416. doi: 10.1021/jm300334d. Epub 2012 Aug 30.

35.

Synthesis and evaluation of eight- and four-membered iminosugar analogues as inhibitors of testicular ceramide-specific glucosyltransferase, testicular β-glucosidase 2, and other glycosidases.

Lee JC, Francis S, Dutta D, Gupta V, Yang Y, Zhu JY, Tash JS, Schönbrunn E, Georg GI.

J Org Chem. 2012 Apr 6;77(7):3082-98. doi: 10.1021/jo202054g. Epub 2012 Mar 20.

36.

Functional consequence of covalent reaction of phosphoenolpyruvate with UDP-N-acetylglucosamine 1-carboxyvinyltransferase (MurA).

Zhu JY, Yang Y, Han H, Betzi S, Olesen SH, Marsilio F, Schönbrunn E.

J Biol Chem. 2012 Apr 13;287(16):12657-67. doi: 10.1074/jbc.M112.342725. Epub 2012 Feb 29.

37.

Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation.

Doi K, Li R, Sung SS, Wu H, Liu Y, Manieri W, Krishnegowda G, Awwad A, Dewey A, Liu X, Amin S, Cheng C, Qin Y, Schonbrunn E, Daughdrill G, Loughran TP Jr, Sebti S, Wang HG.

J Biol Chem. 2012 Mar 23;287(13):10224-35. doi: 10.1074/jbc.M111.334532. Epub 2012 Feb 6.

38.

Fragment-based and structure-guided discovery and optimization of Rho kinase inhibitors.

Li R, Martin MP, Liu Y, Wang B, Patel RA, Zhu JY, Sun N, Pireddu R, Lawrence NJ, Li J, Haura EB, Sung SS, Guida WC, Schonbrunn E, Sebti SM.

J Med Chem. 2012 Mar 8;55(5):2474-8. doi: 10.1021/jm201289r. Epub 2012 Feb 15.

39.

A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A.

Martin MP, Zhu JY, Lawrence HR, Pireddu R, Luo Y, Alam R, Ozcan S, Sebti SM, Lawrence NJ, Schönbrunn E.

ACS Chem Biol. 2012 Apr 20;7(4):698-706. doi: 10.1021/cb200508b. Epub 2012 Jan 27.

40.

Molecular basis of glyphosate resistance-different approaches through protein engineering.

Pollegioni L, Schonbrunn E, Siehl D.

FEBS J. 2011 Aug;278(16):2753-66. doi: 10.1111/j.1742-4658.2011.08214.x. Epub 2011 Jun 28. Review.

41.

Discovery of a potential allosteric ligand binding site in CDK2.

Betzi S, Alam R, Martin M, Lubbers DJ, Han H, Jakkaraj SR, Georg GI, Schönbrunn E.

ACS Chem Biol. 2011 May 20;6(5):492-501. doi: 10.1021/cb100410m. Epub 2011 Feb 22.

42.

The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane.

Berndt N, Yang H, Trinczek B, Betzi S, Zhang Z, Wu B, Lawrence NJ, Pellecchia M, Schönbrunn E, Cheng JQ, Sebti SM.

Cell Death Differ. 2010 Nov;17(11):1795-804. doi: 10.1038/cdd.2010.63. Epub 2010 May 21.

43.

The fungal product terreic acid is a covalent inhibitor of the bacterial cell wall biosynthetic enzyme UDP-N-acetylglucosamine 1-carboxyvinyltransferase (MurA) .

Han H, Yang Y, Olesen SH, Becker A, Betzi S, Schönbrunn E.

Biochemistry. 2010 May 18;49(19):4276-82. doi: 10.1021/bi100365b.

44.

Ack1 mediated AKT/PKB tyrosine 176 phosphorylation regulates its activation.

Mahajan K, Coppola D, Challa S, Fang B, Chen YA, Zhu W, Lopez AS, Koomen J, Engelman RW, Rivera C, Muraoka-Cook RS, Cheng JQ, Schönbrunn E, Sebti SM, Earp HS, Mahajan NP.

PLoS One. 2010 Mar 19;5(3):e9646. doi: 10.1371/journal.pone.0009646.

45.

Structure-based design of high affinity peptides inhibiting the interaction of p53 with MDM2 and MDMX.

Phan J, Li Z, Kasprzak A, Li B, Sebti S, Guida W, Schönbrunn E, Chen J.

J Biol Chem. 2010 Jan 15;285(3):2174-83. doi: 10.1074/jbc.M109.073056. Epub 2009 Nov 12.

46.

Structural basis of glyphosate resistance resulting from the double mutation Thr97 -> Ile and Pro101 -> Ser in 5-enolpyruvylshikimate-3-phosphate synthase from Escherichia coli.

Funke T, Yang Y, Han H, Healy-Fried M, Olesen S, Becker A, Schönbrunn E.

J Biol Chem. 2009 Apr 10;284(15):9854-60. doi: 10.1074/jbc.M809771200. Epub 2009 Feb 11.

47.

Structural characterization of the hemophore HasAp from Pseudomonas aeruginosa: NMR spectroscopy reveals protein-protein interactions between Holo-HasAp and hemoglobin.

Alontaga AY, Rodriguez JC, Schönbrunn E, Becker A, Funke T, Yukl ET, Hayashi T, Stobaugh J, Moënne-Loccoz P, Rivera M.

Biochemistry. 2009 Jan 13;48(1):96-109. doi: 10.1021/bi801860g.

48.

X-ray crystallographic and solution state nuclear magnetic resonance spectroscopic investigations of NADP+ binding to ferredoxin NADP reductase from Pseudomonas aeruginosa.

Wang A, Rodríguez JC, Han H, Schönbrunn E, Rivera M.

Biochemistry. 2008 Aug 5;47(31):8080-93. doi: 10.1021/bi8007356. Epub 2008 Jul 8.

49.

Differential inhibition of class I and class II 5-enolpyruvylshikimate-3-phosphate synthases by tetrahedral reaction intermediate analogues.

Funke T, Healy-Fried ML, Han H, Alberg DG, Bartlett PA, Schönbrunn E.

Biochemistry. 2007 Nov 20;46(46):13344-51. Epub 2007 Oct 25.

PMID:
17958399
50.

Biochemical and structural characterization of Pseudomonas aeruginosa Bfd and FPR: ferredoxin NADP+ reductase and not ferredoxin is the redox partner of heme oxygenase under iron-starvation conditions.

Wang A, Zeng Y, Han H, Weeratunga S, Morgan BN, Moënne-Loccoz P, Schönbrunn E, Rivera M.

Biochemistry. 2007 Oct 30;46(43):12198-211. Epub 2007 Oct 4.

PMID:
17915950

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