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Items: 1 to 50 of 62

1.

A scaffold-hopping approach to discover potent, selective and efficacious inhibitors of NF-κB inducing kinase.

Blaquiere N, Castanedo G, Burch J, Berezhkovskiy L, Brightbill H, Brown S, Chan C, Chiang PC, Crawford JJ, Dong T, Fan P, Feng J, Ghilardi N, Godemann R, Gogol E, Grabbe A, Hole A, Hu B, Hymowitz SG, Alaoui Ismaili MH, Le H, Lee P, Lee W, Lin X, Liu N, McEwan P, McKenzie B, Silvestre H, Suto E, Sujathabhaskar S, Wu G, Wu LC, Zhang Y, Staben ST.

J Med Chem. 2018 Jun 25. doi: 10.1021/acs.jmedchem.8b00678. [Epub ahead of print]

PMID:
29940120
2.

Crystal Structure of Ripk4 Reveals Dimerization-Dependent Kinase Activity.

Huang CS, Oberbeck N, Hsiao YC, Liu P, Johnson AR, Dixit VM, Hymowitz SG.

Structure. 2018 May 1;26(5):767-777.e5. doi: 10.1016/j.str.2018.04.002. Epub 2018 Apr 26.

PMID:
29706531
3.

Targeting the MAPK Pathway in RAS Mutant Cancers.

Hymowitz SG, Malek S.

Cold Spring Harb Perspect Med. 2018 Feb 12. pii: a031492. doi: 10.1101/cshperspect.a031492. [Epub ahead of print]

PMID:
29440321
4.

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).

Castanedo GM, Blaquiere N, Beresini M, Bravo B, Brightbill H, Chen J, Cui HF, Eigenbrot C, Everett C, Feng J, Godemann R, Gogol E, Hymowitz S, Johnson A, Kayagaki N, Kohli PB, Knüppel K, Kraemer J, Krüger S, Loke P, McEwan P, Montalbetti C, Roberts DA, Smith M, Steinbacher S, Sujatha-Bhaskar S, Takahashi R, Wang X, Wu LC, Zhang Y, Staben ST.

J Med Chem. 2017 Jan 26;60(2):627-640. doi: 10.1021/acs.jmedchem.6b01363. Epub 2017 Jan 12.

PMID:
28005357
5.

Unveiling the Structural and Dynamic Nature of the Ubiquitin Code.

Di Lello P, Hymowitz SG.

Structure. 2016 Apr 5;24(4):498-499. doi: 10.1016/j.str.2016.03.013.

6.

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2.

Foster SA, Whalen DM, Özen A, Wongchenko MJ, Yin J, Yen I, Schaefer G, Mayfield JD, Chmielecki J, Stephens PJ, Albacker LA, Yan Y, Song K, Hatzivassiliou G, Eigenbrot C, Yu C, Shaw AS, Manning G, Skelton NJ, Hymowitz SG, Malek S.

Cancer Cell. 2016 Apr 11;29(4):477-493. doi: 10.1016/j.ccell.2016.02.010. Epub 2016 Mar 17.

7.

Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.

René O, Fauber BP, Boenig Gde L, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Kiefer JR, Liimatta M, Lockey P, Norman M, Ouyang W, Wallweber HA, Wong H.

ACS Med Chem Lett. 2014 Dec 4;6(3):276-81. doi: 10.1021/ml500420y. eCollection 2015 Mar 12.

8.

Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.

Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Gallion S, Hymowitz SG, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Maurer B, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Sowell CG, Wang X, Wong H, Xiong JM, Xu J, Zhao Z, Currie KS.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1333-7. doi: 10.1016/j.bmcl.2015.01.032. Epub 2015 Feb 7.

PMID:
25701252
9.

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.

ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 9.

10.

Shining LIGHT on functional promiscuity in the TNF and TNFR superfamilies.

Whalen DM, Hymowitz SG.

Structure. 2014 Sep 2;22(9):1221-1222. doi: 10.1016/j.str.2014.08.003.

11.

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling.

Haling JR, Sudhamsu J, Yen I, Sideris S, Sandoval W, Phung W, Bravo BJ, Giannetti AM, Peck A, Masselot A, Morales T, Smith D, Brandhuber BJ, Hymowitz SG, Malek S.

Cancer Cell. 2014 Sep 8;26(3):402-413. doi: 10.1016/j.ccr.2014.07.007. Epub 2014 Aug 21.

12.

Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.

Fauber BP, René O, de Leon Boenig G, Burton B, Deng Y, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, La H, Liimatta M, Lockey P, Norman M, Ouyang W, Wang W, Wong H.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3891-7. doi: 10.1016/j.bmcl.2014.06.048. Epub 2014 Jun 25.

PMID:
25017032
13.

Dimerization of LTβR by LTα1β2 is necessary and sufficient for signal transduction.

Sudhamsu J, Yin J, Chiang EY, Starovasnik MA, Grogan JL, Hymowitz SG.

Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19896-901. doi: 10.1073/pnas.1310838110. Epub 2013 Nov 18.

14.

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.

Fauber BP, de Leon Boenig G, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Liimatta M, Lockey P, Norman M, Ouyang W, René O, Wong H.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6604-9. doi: 10.1016/j.bmcl.2013.10.054. Epub 2013 Nov 4.

PMID:
24239186
15.

Phosphorylation of Dishevelled by protein kinase RIPK4 regulates Wnt signaling.

Huang X, McGann JC, Liu BY, Hannoush RN, Lill JR, Pham V, Newton K, Kakunda M, Liu J, Yu C, Hymowitz SG, Hongo JA, Wynshaw-Boris A, Polakis P, Harland RM, Dixit VM.

Science. 2013 Mar 22;339(6126):1441-5. doi: 10.1126/science.1232253. Epub 2013 Jan 31.

16.

ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.

Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW.

Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6.

PMID:
23291630
17.

The crystal structure of the catalytic domain of the NF-κB inducing kinase reveals a narrow but flexible active site.

de Leon-Boenig G, Bowman KK, Feng JA, Crawford T, Everett C, Franke Y, Oh A, Stanley M, Staben ST, Starovasnik MA, Wallweber HJ, Wu J, Wu LC, Johnson AR, Hymowitz SG.

Structure. 2012 Oct 10;20(10):1704-14. doi: 10.1016/j.str.2012.07.013. Epub 2012 Aug 23.

18.

Loss of the tumor suppressor BAP1 causes myeloid transformation.

Dey A, Seshasayee D, Noubade R, French DM, Liu J, Chaurushiya MS, Kirkpatrick DS, Pham VC, Lill JR, Bakalarski CE, Wu J, Phu L, Katavolos P, LaFave LM, Abdel-Wahab O, Modrusan Z, Seshagiri S, Dong K, Lin Z, Balazs M, Suriben R, Newton K, Hymowitz S, Garcia-Manero G, Martin F, Levine RL, Dixit VM.

Science. 2012 Sep 21;337(6101):1541-6. Epub 2012 Aug 9.

19.

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ.

J Med Chem. 2012 May 10;55(9):4101-13. doi: 10.1021/jm300060k. Epub 2012 Mar 28.

20.

Phosphorylation-dependent activity of the deubiquitinase DUBA.

Huang OW, Ma X, Yin J, Flinders J, Maurer T, Kayagaki N, Phung Q, Bosanac I, Arnott D, Dixit VM, Hymowitz SG, Starovasnik MA, Cochran AG.

Nat Struct Mol Biol. 2012 Jan 15;19(2):171-5. doi: 10.1038/nsmb.2206.

PMID:
22245969
21.

Engineering and structural characterization of a linear polyubiquitin-specific antibody.

Matsumoto ML, Dong KC, Yu C, Phu L, Gao X, Hannoush RN, Hymowitz SG, Kirkpatrick DS, Dixit VM, Kelley RF.

J Mol Biol. 2012 May 4;418(3-4):134-44. doi: 10.1016/j.jmb.2011.12.053. Epub 2011 Dec 29.

22.

Antagonists induce a conformational change in cIAP1 that promotes autoubiquitination.

Dueber EC, Schoeffler AJ, Lingel A, Elliott JM, Fedorova AV, Giannetti AM, Zobel K, Maurer B, Varfolomeev E, Wu P, Wallweber HJ, Hymowitz SG, Deshayes K, Vucic D, Fairbrother WJ.

Science. 2011 Oct 21;334(6054):376-80. doi: 10.1126/science.1207862.

23.

Preparation of distinct ubiquitin chain reagents of high purity and yield.

Dong KC, Helgason E, Yu C, Phu L, Arnott DP, Bosanac I, Compaan DM, Huang OW, Fedorova AV, Kirkpatrick DS, Hymowitz SG, Dueber EC.

Structure. 2011 Aug 10;19(8):1053-63. doi: 10.1016/j.str.2011.06.010.

24.

Modulation of K11-linkage formation by variable loop residues within UbcH5A.

Bosanac I, Phu L, Pan B, Zilberleyb I, Maurer B, Dixit VM, Hymowitz SG, Kirkpatrick DS.

J Mol Biol. 2011 May 6;408(3):420-31. doi: 10.1016/j.jmb.2011.03.011. Epub 2011 Mar 10.

PMID:
21396940
25.

An Fcγ receptor-dependent mechanism drives antibody-mediated target-receptor signaling in cancer cells.

Wilson NS, Yang B, Yang A, Loeser S, Marsters S, Lawrence D, Li Y, Pitti R, Totpal K, Yee S, Ross S, Vernes JM, Lu Y, Adams C, Offringa R, Kelley B, Hymowitz S, Daniel D, Meng G, Ashkenazi A.

Cancer Cell. 2011 Jan 18;19(1):101-13. doi: 10.1016/j.ccr.2010.11.012.

26.

Regulation and functions of the IL-10 family of cytokines in inflammation and disease.

Ouyang W, Rutz S, Crellin NK, Valdez PA, Hymowitz SG.

Annu Rev Immunol. 2011;29:71-109. doi: 10.1146/annurev-immunol-031210-101312. Review.

PMID:
21166540
27.

Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis.

Di Paolo JA, Huang T, Balazs M, Barbosa J, Barck KH, Bravo BJ, Carano RA, Darrow J, Davies DR, DeForge LE, Diehl L, Ferrando R, Gallion SL, Giannetti AM, Gribling P, Hurez V, Hymowitz SG, Jones R, Kropf JE, Lee WP, Maciejewski PM, Mitchell SA, Rong H, Staker BL, Whitney JA, Yeh S, Young WB, Yu C, Zhang J, Reif K, Currie KS.

Nat Chem Biol. 2011 Jan;7(1):41-50. doi: 10.1038/nchembio.481. Epub 2010 Nov 28.

PMID:
21113169
28.

Ubiquitin binding to A20 ZnF4 is required for modulation of NF-κB signaling.

Bosanac I, Wertz IE, Pan B, Yu C, Kusam S, Lam C, Phu L, Phung Q, Maurer B, Arnott D, Kirkpatrick DS, Dixit VM, Hymowitz SG.

Mol Cell. 2010 Nov 24;40(4):548-57. doi: 10.1016/j.molcel.2010.10.009.

29.

Unleashing cell death: the Fas-FADD complex.

Hymowitz SG, Dixit VM.

Nat Struct Mol Biol. 2010 Nov;17(11):1289-90. doi: 10.1038/nsmb1110-1289. No abstract available.

PMID:
21088666
30.

Interactions between Hedgehog proteins and their binding partners come into view.

Beachy PA, Hymowitz SG, Lazarus RA, Leahy DJ, Siebold C.

Genes Dev. 2010 Sep 15;24(18):2001-12. doi: 10.1101/gad.1951710. Review.

31.

K11-linked polyubiquitination in cell cycle control revealed by a K11 linkage-specific antibody.

Matsumoto ML, Wickliffe KE, Dong KC, Yu C, Bosanac I, Bustos D, Phu L, Kirkpatrick DS, Hymowitz SG, Rape M, Kelley RF, Dixit VM.

Mol Cell. 2010 Aug 13;39(3):477-84. doi: 10.1016/j.molcel.2010.07.001. Epub 2010 Jul 22.

32.

Hedgehog pathway antagonist 5E1 binds hedgehog at the pseudo-active site.

Maun HR, Wen X, Lingel A, de Sauvage FJ, Lazarus RA, Scales SJ, Hymowitz SG.

J Biol Chem. 2010 Aug 20;285(34):26570-80. doi: 10.1074/jbc.M110.112284. Epub 2010 May 26.

33.

Therapeutic antibody targeting of individual Notch receptors.

Wu Y, Cain-Hom C, Choy L, Hagenbeek TJ, de Leon GP, Chen Y, Finkle D, Venook R, Wu X, Ridgway J, Schahin-Reed D, Dow GJ, Shelton A, Stawicki S, Watts RJ, Zhang J, Choy R, Howard P, Kadyk L, Yan M, Zha J, Callahan CA, Hymowitz SG, Siebel CW.

Nature. 2010 Apr 15;464(7291):1052-7. doi: 10.1038/nature08878.

PMID:
20393564
34.

A20: from ubiquitin editing to tumour suppression.

Hymowitz SG, Wertz IE.

Nat Rev Cancer. 2010 May;10(5):332-41. doi: 10.1038/nrc2775. Epub 2010 Apr 12. Review.

PMID:
20383180
35.

Multiple novel classes of APRIL-specific receptor-blocking peptides isolated by phage display.

Gordon NC, Lien S, Johnson J, Wallweber HJ, Tran T, Currell B, Mathieu M, Quan C, Starovasnik MA, Hymowitz SG, Kelley RF.

J Mol Biol. 2010 Feb 12;396(1):166-77. doi: 10.1016/j.jmb.2009.11.041. Epub 2009 Nov 26.

PMID:
19945466
36.

The structure of SHH in complex with HHIP reveals a recognition role for the Shh pseudo active site in signaling.

Bosanac I, Maun HR, Scales SJ, Wen X, Lingel A, Bazan JF, de Sauvage FJ, Hymowitz SG, Lazarus RA.

Nat Struct Mol Biol. 2009 Jul;16(7):691-7. doi: 10.1038/nsmb.1632. Epub 2009 Jun 28.

PMID:
19561609
37.

Antagonism of c-IAP and XIAP proteins is required for efficient induction of cell death by small-molecule IAP antagonists.

Ndubaku C, Varfolomeev E, Wang L, Zobel K, Lau K, Elliott LO, Maurer B, Fedorova AV, Dynek JN, Koehler M, Hymowitz SG, Tsui V, Deshayes K, Fairbrother WJ, Flygare JA, Vucic D.

ACS Chem Biol. 2009 Jul 17;4(7):557-66. doi: 10.1021/cb900083m.

PMID:
19492850
38.

Ubiquitin chain editing revealed by polyubiquitin linkage-specific antibodies.

Newton K, Matsumoto ML, Wertz IE, Kirkpatrick DS, Lill JR, Tan J, Dugger D, Gordon N, Sidhu SS, Fellouse FA, Komuves L, French DM, Ferrando RE, Lam C, Compaan D, Yu C, Bosanac I, Hymowitz SG, Kelley RF, Dixit VM.

Cell. 2008 Aug 22;134(4):668-78. doi: 10.1016/j.cell.2008.07.039.

39.

Structural and functional analysis of the interaction between the agonistic monoclonal antibody Apomab and the proapoptotic receptor DR5.

Adams C, Totpal K, Lawrence D, Marsters S, Pitti R, Yee S, Ross S, Deforge L, Koeppen H, Sagolla M, Compaan D, Lowman H, Hymowitz S, Ashkenazi A.

Cell Death Differ. 2008 Apr;15(4):751-61. doi: 10.1038/sj.cdd.4402306. Epub 2008 Jan 25.

40.

In vivo blockade of OX40 ligand inhibits thymic stromal lymphopoietin driven atopic inflammation.

Seshasayee D, Lee WP, Zhou M, Shu J, Suto E, Zhang J, Diehl L, Austin CD, Meng YG, Tan M, Bullens SL, Seeber S, Fuentes ME, Labrijn AF, Graus YM, Miller LA, Schelegle ES, Hyde DM, Wu LC, Hymowitz SG, Martin F.

J Clin Invest. 2007 Dec;117(12):3868-78.

41.

The mitotic regulator Survivin binds as a monomer to its functional interactor Borealin.

Bourhis E, Hymowitz SG, Cochran AG.

J Biol Chem. 2007 Nov 30;282(48):35018-23. Epub 2007 Sep 19.

42.

Death-receptor O-glycosylation controls tumor-cell sensitivity to the proapoptotic ligand Apo2L/TRAIL.

Wagner KW, Punnoose EA, Januario T, Lawrence DA, Pitti RM, Lancaster K, Lee D, von Goetz M, Yee SF, Totpal K, Huw L, Katta V, Cavet G, Hymowitz SG, Amler L, Ashkenazi A.

Nat Med. 2007 Sep;13(9):1070-7. Epub 2007 Sep 2.

PMID:
17767167
43.

The crystal structure of the costimulatory OX40-OX40L complex.

Compaan DM, Hymowitz SG.

Structure. 2006 Aug;14(8):1321-30.

44.

Delineation of the cell-extrinsic apoptosis pathway in the zebrafish.

Eimon PM, Kratz E, Varfolomeev E, Hymowitz SG, Stern H, Zha J, Ashkenazi A.

Cell Death Differ. 2006 Oct;13(10):1619-30. Epub 2006 Aug 4.

45.

Activation of the proapoptotic death receptor DR5 by oligomeric peptide and antibody agonists.

Li B, Russell SJ, Compaan DM, Totpal K, Marsters SA, Ashkenazi A, Cochran AG, Hymowitz SG, Sidhu SS.

J Mol Biol. 2006 Aug 18;361(3):522-36. Epub 2006 Jul 7.

PMID:
16859704
46.

Synthetic anti-BR3 antibodies that mimic BAFF binding and target both human and murine B cells.

Lee CV, Hymowitz SG, Wallweber HJ, Gordon NC, Billeci KL, Tsai SP, Compaan DM, Yin J, Gong Q, Kelley RF, DeForge LE, Martin F, Starovasnik MA, Fuh G.

Blood. 2006 Nov 1;108(9):3103-11. Epub 2006 Jul 13.

47.

De novo proteomic sequencing of a monoclonal antibody raised against OX40 ligand.

Pham V, Henzel WJ, Arnott D, Hymowitz S, Sandoval WN, Truong BT, Lowman H, Lill JR.

Anal Biochem. 2006 May 1;352(1):77-86. Epub 2006 Feb 21.

PMID:
16545334
48.

Toward small-molecule agonists of TNF receptors.

Hymowitz SG, Ashkenazi A.

Nat Chem Biol. 2005 Dec;1(7):353-4. No abstract available.

PMID:
16370368
49.

Attenuating lymphocyte activity: the crystal structure of the BTLA-HVEM complex.

Compaan DM, Gonzalez LC, Tom I, Loyet KM, Eaton D, Hymowitz SG.

J Biol Chem. 2005 Nov 25;280(47):39553-61. Epub 2005 Sep 16.

50.

Molecular recognition by a binary code.

Fellouse FA, Li B, Compaan DM, Peden AA, Hymowitz SG, Sidhu SS.

J Mol Biol. 2005 May 20;348(5):1153-62. Epub 2005 Apr 1.

PMID:
15854651

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