From transcriptional regulation to drugging the cancer epigenome

by Bradner, James E
Published 2014

BET and BRAF inhibitors act synergistically against BRAF‐mutant melanoma

by Paoluzzi, Luca, Hanniford, Douglas, Sokolova, Elena, Osman, Iman, Darvishian, Farbod, Wang, Jinhua, Bradner, James E., Hernando, Eva
Published 2016

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

by Spencer, John, Amin, Jahangir, Wang, Minghua, Packham, Graham, Alwi, Sharifah S. Syed, Tizzard, Graham J., Coles, Simon J., Paranal, Ronald M., Bradner, James E., Heightman, Tom D.
Published 2011

Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells

by Fowler, Trent, Ghatak, Payel, Price, David H., Conaway, Ronald, Conaway, Joan, Chiang, Cheng-Ming, Bradner, James E., Shilatifard, Ali, Roy, Ananda L.
Published 2014

Correction: Regulation of MYC Expression and Differential JQ1 Sensitivity in Cancer Cells

by Fowler, Trent, Ghatak, Payel, Price, David H., Conaway, Ronald, Conaway, Joan, Chiang, Cheng-Ming, Bradner, James E., Shilatifard, Ali, Roy, Ananda L.
Published 2015

Targeting the epigenetic readers in Ewing Sarcoma inhibits the oncogenic transcription factor EWS/Fli1

by Jacques, Camille, Lamoureux, François, Baud’huin, Marc, Calleja, Lidia Rodriguez, Quillard, Thibaut, Amiaud, Jérôme, Tirode, Franck, Rédini, Françoise, Bradner, James E., Heymann, Dominique, Ory, Benjamin
Published 2016

HEXIM1 induction is mechanistically involved in mediating anti-AML activity of BET protein bromodomain antagonist

by Devaraj, Santhana G. T., Fiskus, Warren, Shah, Bhavin, Qi, Jun, Sun, Baohua, Iyer, Swaminathan P, Sharma, Sunil, Bradner, James E., Bhalla, Kapil N.
Published 2015

Design and Characterization of Bivalent BET Inhibitors

by Tanaka, Minoru, Roberts, Justin M., Seo, Hyuk-Soo, Souza, Amanda, Paulk, Joshiawa, Scott, Thomas G., DeAngelo, Stephen L., Dhe-Paganon, Sirano, Bradner, James E.
Published 2016

Targeting chromatin binding regulation of constitutively active AR variants to overcome prostate cancer resistance to endocrine-based therapies

by Chan, Siu Chiu, Selth, Luke A., Li, Yingming, Nyquist, Michael D., Miao, Lu, Bradner, James E., Raj, Ganesh V., Tilley, Wayne D., Dehm, Scott M.
Published 2015

Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6

by Hu, Yu-Jie, Belaghzal, Houda, Hsiao, Wen-Yu, Qi, Jun, Bradner, James E., Guertin, David A., Sif, Saïd, Imbalzano, Anthony N.
Published 2015

Small-Molecule Inhibition of BRDT for Male Contraception

by Matzuk, Martin M., McKeown, Michael R., Filippakopoulos, Panagis, Li, Qinglei, Ma, Lang, Agno, Julio E., Lemieux, Madeleine E., Picaud, Sarah, Yu, Richard N., Qi, Jun, Knapp, Stefan, Bradner, James E.
Published 2012

Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML)

by Herrmann, Harald, Blatt, Katharina, Shi, Junwei, Gleixner, Karoline V., Cerny-Reiterer, Sabine, Müllauer, Leonhard, Vakoc, Christopher R., Sperr, Wolfgang R., Horny, Hans-Peter, Bradner, James E., Zuber, Johannes, Valent, Peter
Published 2012

HDAC2 negatively regulates memory formation and synaptic plasticity

by Guan, Ji-Song, Haggarty, Stephen J., Giacometti, Emanuela, Dannenberg, Jan-Hermen, Joseph, Nadine, Gao, Jun, Nieland, Thomas J.F., Zhou, Ying, Wang, Xinyu, Mazitschek, Ralph, Bradner, James E., DePinho, Ronald A., Jaenisch, Rudolf, Tsai, Li-Huei
Published 2009

An oncogenic Ezh2 mutation cooperates with particular genetic alterations to induce tumors in mice and redistributes H3K27 trimethylation throughout the genome

by Souroullas, George P., Jeck, William R., Parker, Joel S., Simon, Jeremy M., Liu, Jie-Yu, Paulk, Joshiawa, Xiong, Jessie, Clark, Kelly S., Fedoriw, Yuri, Qi, Jun, Burd, Christin E., Bradner, James E., Sharpless, Norman E.
Published 2016

Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement

by Yi, Joanna S., Federation, Alexander J., Qi, Jun, Dhe-Paganon, Sirano, Hadler, Michael, Xu, Xiang, St. Pierre, Roodolph, Varca, Anthony C., Wu, Lei, Marineau, Jason J., Smith, William B., Souza, Amanda, Chory, Emma J., Armstrong, Scott A., Bradner, James E.
Published 2014

Dose-dependent role of the cohesin complex in normal and malignant hematopoiesis

by Viny, Aaron D., Ott, Christopher J., Spitzer, Barbara, Rivas, Martin, Meydan, Cem, Papalexi, Efthymia, Yelin, Dana, Shank, Kaitlyn, Reyes, Jaime, Chiu, April, Romin, Yevgeniy, Boyko, Vitaly, Thota, Swapna, Maciejewski, Jaroslaw P., Melnick, Ari, Bradner, James E., Levine, Ross L.
Published 2015

Genome-wide determination of drug localization

by Anders, Lars, Guenther, Matthew G., Qi, Jun, Fan, Zi Peng, Marineau, Jason J., Rahl, Peter B., Lovén, Jakob, Sigova, Alla A., Smith, William B., Lee, Tong Ihn, Bradner, James E., Young, Richard A.
Published 2013

Biased Multicomponent Reactions to Develop Novel Bromodomain Inhibitors

by McKeown, Michael R, Shaw, Daniel L, Fu, Harry, Liu, Shuai, Xu, Xiang, Marineau, Jason J, Huang, Yibo, Zhang, Xiaofeng, Buckley, Dennis L, Kadam, Asha, Zhang, Zijuan, Blacklow, Stephen C, Qi, Jun, Zhang, Wei, Bradner, James E
Published 2014

Notch inhibition allows oncogene independent generation of iPS cells

by Ichida, Justin K., TCW, Julia, Williams, Luis A., Carter, Ava C., Shi, Yingxiao, Moura, Marcelo T., Ziller, Michael, Singh, Sean, Amabile, Giovanni, Bock, Christoph, Umezawa, Akihiro, Rubin, Lee L., Bradner, James E., Akutsu, Hidenori, Meissner, Alexander, Eggan, Kevin
Published 2014

Identification of bromodomain-containing protein 4 (BRD4) as a novel marker and epigenetic target in mast cell leukemia

by Wedeh, Ghaith, Cerny-Reiterer, Sabine, Eisenwort, Gregor, Herrmann, Harald, Blatt, Katharina, Hadzijusufovic, Emir, Sadovnik, Irina, Müllauer, Leonhard, Schwaab, Juliana, Hoffmann, Thomas, Bradner, James E., Radia, Deepti, Sperr, Wolfgang R., Hoermann, Gregor, Reiter, Andreas, Horny, Hans-Peter, Zuber, Johannes, Arock, Michel, Valent, Peter
Published 2015