Selected Publications

Selective HDAC1/HDAC2 Inhibitors Induce Neuroblastoma Differentiation.
Stacey M. Frumm, Zi Peng Fan, Kenneth N. Ross, Jeremy R. Duvall, Supriya Gupta, Lynn VerPlank, Byung-Chul Suh, Edward Holson, Florence F. Wagner, William B. Smith, Ronald M. Paranal, Christopher F. Bassil, Jun Qi, Giovanni Roti, Andrew L. Kung, James E. Bradner, Nicola Tolliday, Kimberly Stegmaier
Chemistry & Biology (23 May 2013, Vol. 20, Issue 5, pp. 713-725)

MYC, a downstream target of BRD-NUT, is necessary and sufficient for the blockade of differentiation in NUT midline carcinoma.
Grayson, A.R., Walsh, E.M., Cameron, M.J., Godec, J., Ashworth, T., Ambrose, J.M., Aserlind, A.B., Wang, H., Evan, G.I., Kluk, M.J., Bradner, J.E., Aster, J.C., French, C.A.
Oncogene (2013) EPub ahead of print.

Transcriptional Amplification in Tumor Cells with Elevated c-Myc
Charles Y. Lin, Jakob Loven, Peter B. Rahl, Ronald M. Paranal, Christopher B. Burge, James E. Bradner, Tong Ihn Lee, and Richard A. Young*
*Corresponding authors. Cell. 26 August 2012; In press.

Small-molecule inhibition of BRDT for male contraception
Matzuk MM*, McKeown MR, Filippakopoulos P, Li Q, Ma L, Ango JE, Lemieux ME, Picaud S, Yu RN, Qi J, Knapp S, Bradner JE*.
*Corresponding authors. Cell. 17 August 2012; In press.

As featured in Cell
As featured in Science
As featured by Nature
As featured by Nature Medicine
As featured by The Atlantic
As featured in The Boston Globe
As featured by The Economist
As featured by US News & World Report
As featured on CNN

BET bromodomain inhibition targets both c-MYC and IL7R in high-risk acute lymphoblastic leukemia
Christopher J. Ott, Nadja Kopp, Liat Bird, Ronald M. Paranal, Jun Qi, Teresa Bowman, Scott J. Rodig, Andrew L. Kung, James E. Bradner* and David M. Weinstock*.
*Corresponding Authors. Blood. 2012 Aug 17. [Epub ahead of print]

Preclinical activity, pharmacodynamic and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.
Santo L, Hideshima T, Kung AL, Tseng JC, Tamang D, Yang M, Jarpe M, van Duzer JH, Mazitschek R, Ogier WC, Cirstea D, Rodig S, Eda H, Scullen T, Canavese M,Bradner, J. E., Anderson KC, Jones SS, Raje N.
Blood. 2012 Jan 19. [Epub ahead of print]

BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc.
Delmore, J. E., Issa, G. C., Lemieux, M. E., Rahl, P. B., Shi, J., Jacobs, H. M., Kastritis, E., Gilpatrick, T., Paranal, R. M., Qi, J., Chesi, M., Schinzel, A. C., McKeown, M. R., Heffernan, T. P., Vakoc, C. R., Bergsagel, P. L., Ghobrial, I. M., Richardson, P. G., Young, R. A., Hahn, W. C., Anderson, K. C., Kung, A. L., Bradner, J. E.*, Mitsiades, C. S*.
Cell. 2011 Sep 16;146(6):904-17. Epub 2011 Sep 1. *Corresponding authors

As featured in Nature Chem Bio
As featured in Nature Reviews Drug Discovery
As featured in Nature Reviews Cancer
As featured in ACS Chem Bio
As featured in Nature Medicine
As featured in Nature Medicine
As featured in The Economist
As featured in SciBX

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.
Zuber J, Shi J, Wang E, Rappaport AR, Herrmann H, Sison EA, Magoon D, Qi J, Blatt K, Wunderlich M, Taylor MJ, Johns C, Chicas A, Mulloy JC, Kogan SC, Brown P, Valent P, Bradner JE, Lowe SW, Vakoc CR.
Nature. 2011 Aug 3. doi: 10.1038/nature10334. [Epub ahead of print]

As featured in Nature Reviews Cancer
As featured in SciBX
As featured in Cancer Cell
As featured in Cancer Research
As featured in The New England Journal of Medicine

Differentiation of NUT Midline Carcinoma in Humans and Mice by Epigenomic Reprogramming
Schwartz, B. E., Hofer, M. D., Lemieux, M. E., Bauer, D. E., Cameron, M. J., West, N. H., Agoston, E. S., Reynoird, N., Khochbin, S., Ince, T. A., Christie, A., Janeway, K. A., Vargas, S. O., Perez-Atayde, A. R., Aster, J. C., Sallan, S. E., Kung, A. L., Bradner, J. E., French, C. A.
Cancer Research - Published OnlineFirst March 31, 2011;

Selective inhibition of BET bromodomains.
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* and Bradner JE*.
Nature. 2010 Sep 24 [Epub ahead of print]; 468:1067-73 *Corresponding authors

As featured in SciBX
As featured in Chemical & Engineering News
As featured in ACS Chemical Biology
As featured in Nature
As featured in Angewandte Chemie
As featured in SciBX
As featured in Cancer Research
As featured in Financial Times
As featured in Nature Reviews Drug Discovery
As featured in The New England Journal of Medicine

HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans.
Marubayashi S, Koppikar P, Taldone T, Abdel-Wahab O, West N, Bhagwat N, Caldas-Lopes E, Ross KN, Gonen M, Gozman A, Ahn JH, Rodina A, Ouerfelli O, Yang G, Hedvat C, Bradner JE*, Chiosis G*, Levine RL*.
J Clin Invest. 2010 Sep 13. pii: 42442. *Corresponding authors
As featured in SciBX. 2010 Sept 30; doi:10.1038/scibx.2010.1138.

Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease.
Bradner JE, Mak R, Tanguturi SK, Mazitschek R, Haggarty SJ, Ross K, Chang CY, Bosco J, West N, Morse E, Lin K, Shen JP, Kwiatkowski NP, Gheldof N, Dekker J, DeAngelo DJ, Carr SA, Schreiber SL, Golub TR, Ebert BL.
Proc Natl Acad Sci U S A. 2010 Jul 13;107(28):12617-22. Epub 2010 Jun 28.

Chemical phylogenetics of histone deacetylases.
Bradner JE*, West N, Grachan ML, Greenberg EF, Haggarty SJ, Warnow T and Mazitschek R*.
Nature Chemical Biology. 2010 Feb 7; Advance online publication. *Corresponding authors

Direct inhibition of the NOTCH transcription factor complex.
Moellering RE, Cornejo M, Davis TN, Del Bianco C, Aster JC, Blacklow SC, Kung AL, Gilliland DG, Verdine GL and Bradner JE.
Nature. 2009 Nov 12; 462: 182-188.
As featured in Nature. 2009 Nov 12; 462:171-172.
As featured in Chemical & Engineering News. 2009 Nov 16; 87(46):9.
As featured in Science Signaling. 2009 Nov 17; 2:ec369.
As featured in Developmental Cell. 2009 Dec 15; 17(6):750-2.
As featured in ACS Chemical Biology. 2009 Dec 18; 4(12):975-8.

Donor-recipient mismatch for common gene deletion polymorphisms in graft-versus-host disease.
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 and Altshuler D.
Nature Genetics. 22 November 2009; 41(12):1341-4.
As featured in Nature Genetics. 2009 41:1263-4.

HDAC2 negatively regulates memory formation and synaptic plasticity.
Guan JS, Haggarty SJ, Giacometti E, Dannenberg JH, Joseph N, Gao J, Nieland TJ, Zhou Y, Wang X, Mazitschek R, Bradner JE, DePinho RA, Jaenisch R, Tsai LH.
Nature. 2009; 459(7243):55-60.

A pulse at the heart of targeted therapy
Bradner JE
Nature Chemical Biology. 2009;5(3):144-5.

Identification and characterization of small molecule inhibitors of a class I histone deacetylase from Plasmodium falciparum.
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.
Journal of Medicinal Chemistry. 2009;52(8):2185-7.

Synthesis and HDAC Inhibitory Activity of Largazole Analogs: Alteration of the Zinc-Binding Domain and Macrocyclic Scaffold.
Bowers A, West N, Newkirk TL, Troutman-Youngman AE, Schreiber SL, Bradner JE* and Williams RM*.
Organic Letters. 2009;11(6):1301-4.

Synthesis and Conformation-Activity Relationships of the Peptide Isosteres of FK228 and Largazole.
Bowers A, Greshock TJ, West N, Estiu G, Schreiber SL, Wiest O, Williams RM and Bradner JE.
Journal of the American Chemical Society. 2009 Feb 4.

The Total Synthesis and Biological Mode of Action of Largazole: A Potent Class I Histone Deacetylase (HDAC) Inhibitor.
Bowers A, West N, Taunton J, Schreiber SL, Bradner JE and Williams RM.
Journal of the American Chemical Society. 2008 Aug 20;130(33):11219-22. Epub 2008 Jul 19.

On the Structural Origin of Selectivity in Class II-Selective Histone Deacetylase Inhibitors.
Estiu G, Greenberg EF, Harrison CB, Mazitschek R, Bradner JE and Wiest O.
Journal of Medicinal Chemistry. 2008;51(10):2898-906.

Coactivation of Receptor Tyrosine Kinases Affects the Response of Tumor Cells to Targeted Therapies.
Stommel JM, Kimmelman AC, Ying H, Nabioullin R, Ponugoti AH, Wiedemeyer R, Stegh AH, Bradner JE, Ligon KL, Brennan C, Chin L, Depinho RA.
Science. 2007;318(5848):287-90.

Fluorous-Based Small-Molecule Microarrays for the Discovery of Histone Deacetylase Inhibitors.
Vegas AJ, Bradner JE, Tang W, McPherson OM, Greenberg EF, Koehler AN, Schreiber SL.
Angewandte Chemie. 2007;46(42):7960-4.
As featured in Angew Chem Int Ed Engl. 2008;47:2-5.

A Method for the Covalent Capture and Screening of Diverse Small Molecules in a Microarray Format.
Bradner JE, McPherson OM, Koehler AN.
Nature Protocols. 2006;1(5):2344-52.

A robust small-molecule microarray platform for screening cell lysates.
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.
Chemistry & Biology. 2006;13(5):493-504.
As featured in Nature Biotechnology 2006; 24: 799.

Small-molecule inhibition of proteasome and aggresome function induces synergistic antitumor activity in multiple myeloma.
Hideshima T, Bradner JE, Wong J, Chauhan D, Richardson P, Schreiber SL, Anderson KC.
Proceedings of the National Academy of Sciences 2005; 102: 8567-72.

DNA-bend modulation in a repressor-to-activator switching mechanism.
Ansari AZ, Bradner JE and O'Halloran TV
Nature. 374:371-375, 1995.