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James E. Bradner, MD

Publications

  • Amin J, Puglisi A, Clarke J, Milton J, Wang M, Paranal RM, Bradner JE, Spencer J.A cyclodextrin-capped histone deacetylase inhibitor.Bioorg Med Chem Lett. 2013 Apr 2.
    23591111
  • Lovén J, Hoke HA, Lin CY, Lau A, Orlando DA, Vakoc CR, Bradner JE, Lee TI, Young RA.Selective inhibition of tumor oncogenes by disruption of super-enhancers.Cell. 2013 Apr 11;153(2):320-34.
    23582323
  • Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Muller S, Schwaller J, Stankovic T, Knapp S.PFI-1 - A highly Selective Protein Interaction Inhibitor Targeting BET bromodomains.Cancer Res. 2013 Apr 10.
    23576556
  • Wang X, Helfer CM, Pancholi N, Bradner JE, You J.Recruitment of Brd4 to the human papillomavirus type 16 DNA replication complex is essential for replication of viral DNA.J Virol. 2013 Apr;87(7):3871-84.
    23365439
  • Puissant A, Frumm SM, Alexe G, Bassil CF, Qi J, Chanthery YH, Nekritz EA, Zeid R, Gustafson WC, Greninger P, Garnett MJ, McDermott U, Benes CH, Kung AL, Weiss WA, Bradner JE, Stegmaier K.Targeting MYCN in neuroblastoma by BET bromodomain inhibition.Cancer Discovery. 2013 Mar;3(3):308-23.
    23430699
  • Herrmann H, Blatt K, Shi J, Gleixner KV, Cerny-Reiterer S, Müllauer L, Vakoc CR, Sperr WR, Horny HP, Bradner JE, Zuber J, Valent P.Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia AML.Oncotarget. 2012 Dec;3(12):1588-99.
    23249862
  • Gao C, Dimitrov T, Yong KJ, Tatetsu H, Jeong HW, Luo HR, Bradner JE, Tenen DG, Chai L.Targeting transcription factor SALL4 in acute myeloid leukemia by interrupting its interaction with an epigenetic complex.Blood. 2013 Feb 21;121(8):1413-21.
    23287862
  • Yu W, Chory EJ, Wernimont AK, Tempel W, Scopton A, Federation A, Marineau JJ, Qi J, Barsyte-Lovejoy D, Yi J, Marcellus R, Iacob RE, Engen JR, Griffin C, Aman A, Wienholds E, Li F, Pineda J, Estiu G, Shatseva T, Hajian T, Al-Awar R, Dick JE, Vedadi M, Brown PJ, Arrowsmith CH, Bradner JE, Schapira M.Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.Nat Commun. 2012;3:1288.
    23250418
  • Lockwood WW, Zejnullahu K, Bradner JE, Varmus H.Sensitivity of human lung adenocarcinoma cell lines to targeted inhibition of BET epigenetic signaling proteins.Proc Natl Acad Sci U S A. 2012 Nov 20;109(47):19408-13.
    23129625
  • Deshpande AJ, Bradner J, Armstrong SA.Chromatin modifications as therapeutic targets in MLL-rearranged leukemia.Trends Immunol. 2012 Nov;33(11):563-70.
    22867873
  • Bauer DE, Mitchell CM, Strait KM, Lathan CS, Stelow EB, Lüer SC, Muhammed S, Evans AG, Sholl LM, Rosai J, Giraldi E, Oakley RP, Rodriguez-Galindo C, London WB, Sallan SE, Bradner JE, French CA.Clinicopathologic Features and Long-term Outcomes of NUT Midline Carcinoma.Clin Cancer Res. 2012 Oct 15;18(20):5773-5779.
    22896655
  • Ott CJ, Kopp N, Bird L, Paranal RM, Qi J, Bowman T, Rodig SJ, Kung AL, Bradner JE, Weinstock DM.BET bromodomain inhibition targets both c-Myc and IL7R in high-risk acute lymphoblastic leukemia.Blood. 2012 Oct 4;120(14):2843-52.
    22904298
  • Lin CY, Lovén J, Rahl PB, Paranal RM, Burge CB, Bradner JE, Lee TI, Young RA.Transcriptional amplification in tumor cells with elevated c-Myc.Cell. 2012 Sep 28;151(1):56-67.
    23021215
  • Wen Q, Goldenson B, Silver SJ, Schenone M, Dancik V, Huang Z, Wang LZ, Lewis TA, An WF, Li X, Bray MA, Thiollier C, Diebold L, Gilles L, Vokes MS, Moore CB, Bliss-Moreau M, Verplank L, Tolliday NJ, Mishra R, Vemula S, Shi J, Wei L, Kapur R, Lopez CK, Gerby B, Ballerini P, Pflumio F, Gilliland DG, Goldberg L, Birger Y, Izraeli S, Gamis AS, Smith FO, Woods WG, Taub J, Scherer CA, Bradner JE, Goh BC, Mercher T, Carpenter AE, Gould RJ, Clemons PA, Carr SA, Root DE, Schreiber SL, Stern AM, Crispino JD.Identification of regulators of polyploidization presents therapeutic targets for treatment of AMKL.Cell. 2012 Aug 3;150(3):575-89.
    22863010
  • Schwartz BE, Hofer MD, Lemieux ME, Bauer DE, Cameron MJ, West NH, Agoston ES, Reynoird N, Khochbin S, Ince TA, Christie A, Janeway KA, Vargas SO, Perez-Atayde AR, Aster JC, Sallan SE, Kung AL, Bradner JE, French CA.Differentiation of NUT Midline Carcinoma by Epigenomic Reprogramming.Cancer Res. 2011 Apr 1;71(7):2686-96.
    21447744
  • de Zoeten EF, Wang L, Butler K, Beier UH, Akimova T, Sai H, Bradner JE, Mazitschek R, Kozikowski AP, Matthias P, Hancock WW.HDAC6 and HSP90 Control The Functions Of Foxp3+ T-Regulatory Cells.Mol Cell Biol. 2011 Mar 28.
    21444725
  • Tang W, Luo T, Greenberg EF, Bradner JE, Schreiber SL.Discovery of histone deacetylase 8 selective inhibitors.Bioorg Med Chem Lett. 2011 Feb 2.
    21334896
  • Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE.Selective inhibition of BET bromodomains.Nature. 2010 Dec 23;468(7327):1067-73.
    20871596
  • Marubayashi S, Koppikar P, Taldone T, Abdel-Wahab O, West N, Bhagwat N, Caldas-Lopes E, Ross KN, Gönen M, Gozman A, Ahn JH, Rodina A, Ouerfelli O, Yang G, Hedvat C, Bradner JE, Chiosis G, Levine RL.HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans.J Clin Invest. 2010 Oct 1;120(10):3578-93.
    20852385
  • Bowers AA,Greshock TJ,West N,Estiu G,Schreiber SL,Wiest O,Williams RM,Bradner JE.Synthesis and Conformation-Activity Relationships of the Peptide Isosteres of FK228 and Largazole.J Am Chem Soc. 2009 Mar 4;131(8):2900-5.
    19193120
  • Estiu G, West N, Mazitschek R, Greenberg E, Bradner JE, Wiest O.On the inhibition of histone deacetylase 8.Bioorg Med Chem. 2010 Jun 1;18(11):4103-10.
    20472442
  • Bradner JE, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T, Mazitschek R.Chemical phylogenetics of histone deacetylases.Nat Chem Biol. 2010 Mar;6(3):238-243.
    20139990
  • Yoda A, Yoda Y, Chiaretti S, Bar-Natan M, Mani K, Rodig SJ, West N, Xiao Y, Brown JR, Mitsiades C, Sattler M, Kutok JL, DeAngelo DJ, Wadleigh M, Piciocchi A, Dal Cin P, Bradner JE, Griffin JD, Anderson KC, Stone RM, Ritz J, Foà R, Aster JC, Frank DA, Weinstock DM.Functional screening identifies CRLF2 in precursor B-cell acute lymphoblastic leukemia.Proc Natl Acad Sci U S A. 2010 Jan 5;107(1):252-7.
    20018760
  • McCarroll SA, Bradner JE, Turpeinen H, Volin L, Martin PJ, Chilewski SD, Antin JH, Lee SJ, Ruutu T, Storer B, Warren EH, Zhang B, Zhao LP, Ginsburg D, Soiffer RJ, Partanen J, Hansen JA, Ritz J, Palotie A, Altshuler D.Donor-recipient mismatch for common gene deletion polymorphisms in graft-versus-host disease.Nat Genet. 2009 Dec;41(12):1341-4.
    19935662
  • Moellering RE, Cornejo M, Davis TN, Del Bianco C, Aster JC, Blacklow SC, Kung AL, Gilliland DG, Verdine GL, Bradner JE.Direct inhibition of the NOTCH transcription factor complex.Nature. 2009 Nov 12;462(7270):182-8.
    19907488
  • Kimbrel EA, Davis TN, Bradner JE, Kung AL.In vivo pharmacodynamic imaging of proteasome inhibition.Mol Imaging.;8(3):140-7.
    19723471
  • Moellering RE, Cornejo M, Davis TN, Del Bianco C, Aster JC, Blacklow SC, Kung AL, Gilliland DG, Verdine GL, Bradner J.Direct inhibition of the Notch transcription factor complex.Nature..
  • Kawada J,Zou P,Mazitschek R,Bradner JE,Cohen JI.Tubacin kills Epstein-Barr virus (EBV)-Burkitt lymphoma cells by inducing reactive oxygen species and EBV lymphoblastoid cells by inducing apoptosis.J Biol Chem. 2009 Jun 19;284(25):17102-9.
    19386607
  • Patel V,Mazitschek R,Coleman B,Nguyen C,Urgaonkar S,Cortese J,Barker RH,Greenberg E,Tang W,Bradner JE,Schreiber SL,Duraisingh MT,Wirth DF,Clardy J.Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.J Med Chem. 2009 Apr 23;52(8):2185-7.
    19317450
  • Bowers AA,West N,Newkirk TL,Troutman-Youngman AE,Schreiber SL,Wiest O,Bradner JE,Williams RM.Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.Org Lett. 2009 Mar 19;11(6):1301-4.
    19239241
  • Bradner JE.A pulse at the heart of targeted therapy.Nat Chem Biol. 2009 Mar;5(3):144-5.
    19219016
  • Bowers A,West N,Taunton J,Schreiber SL,Bradner JE,Williams RM.Total synthesis and biological mode of action of largazole: a potent class I histone deacetylase inhibitor.J Am Chem Soc. 2008 Aug 20;130(33):11219-22.
    18642817
  • Estiu G, Greenberg E, Harrison CB, Kwiatkowski NP, Mazitschek R, Bradner JE, Wiest O.Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors.J Med Chem. 2008 May 22;51(10):2898-906.
    18412327
  • Engelman JA, Zejnullahu K, Gale CM, Lifshits E, Gonzales AJ, Shimamura T, Zhao F, Vincent PW, Naumov GN, Bradner JE, Althaus IW, Gandhi L, Shapiro GI, Nelson JM, Heymach JV, Meyerson M, Wong KK, Jnne PA.PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.Cancer Res. 2007 Dec 15;67(24):11924-32.
    18089823
  • Stommel JM, Kimmelman AC, Ying H, Nabioullin R, Ponugoti AH, Wiedemeyer R, Stegh AH, Bradner JE, Ligon KL, Brennan C, Chin L, DePinho RA.Coactivation of receptor tyrosine kinases affects the response of tumor cells to targeted therapies.Science. 2007 Oct 12;318(5848):287-90.
    17872411
  • Duan Z, Bradner J, Greenberg E, Mazitschek R, Foster R, Mahoney J, Seiden MV.8-benzyl-4-oxo-8-azabicyclo[3.2.1]oct-2-ene-6,7-dicarboxylic acid (SD-1008), a novel janus kinase 2 inhibitor, increases chemotherapy sensitivity in human ovarian cancer cells.Mol Pharmacol. 2007 Nov;72(5):1137-45.
    17675586
  • Bradner JE, McPherson OM, Koehler AN.A method for the covalent capture and screening of diverse small molecules in a microarray format.Nat Protoc. 2006;1(5):2344-52.
    17406478
  • Bradner JE, McPherson OM, Mazitschek R, Barnes-Seeman D, Shen JP, Dhaliwal J, Stevenson KE, Duffner JL, Park SB, Neuberg DS, Nghiem P, Schreiber SL, Koehler AN.A robust small-molecule microarray platform for screening cell lysates.Chem Biol. 2006 May;13(5):493-504.
    16720270
  • Hideshima T, Bradner JE, Wong J, Chauhan D, Richardson P, Schreiber SL, Anderson KC.Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma.Proc Natl Acad Sci U S A. 2005 Jun 14;102(24):8567-72.
    15937109
  • Ansari AZ, Bradner JE, O'Halloran TV.DNA-bend modulation in a repressor-to-activator switching mechanism.Nature. 1995 Mar 23;374(6520):371-5.
    7885478