Now showing items 21-29 of 29

    • Response and resistance to BET bromodomain inhibitors in triple negative breast cancer 

      Shu, Shaokun; Lin, Charles Y.; He, Housheng Hansen; Witwicki, Robert M.; Tabassum, Doris P.; Roberts, Justin M.; Janiszewska, Michalina; Huh, Sung Jin; Liang, Yi; Ryan, Jeremy; Doherty, Ernest; Mohammed, Hisham; Guo, Hao; Stover, Daniel G.; Ekram, Muhammad B.; Brown, Jonathan; D'Santos, Clive; Krop, Ian E.; Dillon, Deborah; McKeown, Michael; Ott, Christopher; Qi, Jun; Ni, Min; Rao, Prakash K.; Duarte, Melissa; Wu, Shwu-Yuan; Chiang, Cheng-Ming; Anders, Lars; Young, Richard A.; Winer, Eric; Letai, Antony; Barry, William T.; Carroll, Jason S.; Long, Henry; Brown, Myles; Liu, X. Shirley; Meyer, Clifford A.; Bradner, James E.; Polyak, Kornelia (2015)
      Triple negative breast cancer (TNBC) is a heterogeneous and clinically aggressive disease for which there is no targeted therapy1-3. BET bromodomain inhibitors, which have shown efficacy in several models of cancer4-6, ...
    • Small-molecule inhibition of BRD4 as a new potent approach to eliminate leukemic stem- and progenitor cells in acute myeloid leukemia (AML) 

      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 (Impact Journals LLC, 2012)
      Acute myeloid leukemia (AML) is a life-threatening stem cell disease characterized by uncontrolled proliferation and accumulation of myeloblasts. Using an advanced RNAi screen-approach in an AML mouse model we have recently ...
    • Structure-Guided DOT1L Probe Optimization by Label-Free Ligand Displacement 

      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. (American Chemical Society, 2014)
      The DOT1L lysine methyltransferase has emerged as a validated therapeutic target in MLL-rearranged (MLLr) acute leukemias. Although S-adenosylmethionine competitive inhibitors have demonstrated pharmacological proof-of-principle ...
    • Targeting STAT5 in Hematologic Malignancies through Inhibition of the Bromodomain and Extra-Terminal (BET) Bromodomain Protein BRD2 

      Liu, Suhu; Walker, Sarah Rebecca; Nelson, E; Cerulli, R.; Xiang, Michael; Toniolo, P. A.; Qi, Jun; Stone, Richard Maury; Wadleigh, Martha; Bradner, James Elliott; Frank, David Alan (American Association for Cancer Research (AACR), 2014)
      The transcription factor signal STAT5 is constitutively activated in a wide range of leukemias and lymphomas, and drives the expression of genes necessary for proliferation, survival, and self-renewal. Thus, targeting STAT5 ...
    • Targeting the epigenetic readers in Ewing Sarcoma inhibits the oncogenic transcription factor EWS/Fli1 

      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 (Impact Journals LLC, 2016)
      Ewing Sarcoma is a rare bone and soft tissue malignancy affecting children and young adults. Chromosomal translocations in this cancer produce fusion oncogenes as characteristic molecular signatures of the disease. The ...
    • Targeting Transcription Factor SALL4 in Acute Myeloid Leukemia by Interrupting Its Interaction with an Epigenetic Complex 

      Gao, Chong; Dimitrov, Todor; Yong, Kol Jia; Tatetsu, Hiro; Jeong, Ha-Won; Luo, Hongbo; Bradner, James Elliott; Tenen, Daniel Geoffrey; Chai, Li (American Society of Hematology, 2013)
      An exciting recent approach to targeting transcription factors in cancer is to block formation of oncogenic complexes. We investigated whether interfering with the interaction of the transcription factor SALL4, which is ...
    • Transcriptional and post-transcriptional control of adipocyte differentiation by Jumonji domain-containing protein 6 

      Hu, Yu-Jie; Belaghzal, Houda; Hsiao, Wen-Yu; Qi, Jun; Bradner, James E.; Guertin, David A.; Sif, Saïd; Imbalzano, Anthony N. (Oxford University Press, 2015)
      Jumonji domain-containing protein 6 (JMJD6) is a nuclear protein involved in histone modification, transcription and RNA processing. Although JMJD6 is crucial for tissue development, the link between its molecular functions ...
    • Triplication of a 21q22 region contributes to B cell transformation through HMGN1 overexpression and loss of histone H3 lysine 27 trimethylation 

      Lane, Andrew A.; Chapuy, Bjoern; Lin, Charles Y.; Tivey, Trevor; Li, Hubo; Townsend, Elizabeth C.; van Bodegom, Diederik; Day, Tovah A.; Wu, Shuo-Chieh; Liu, Huiyun; Yoda, Akinori; Alexe, Gabriela; Schinzel, Anna C.; Sullivan, Timothy J.; Malinge, Sébastien; Taylor, Jordan E.; Stegmaier, Kimberly; Jaffe, Jacob D.; Bustin, Michael; te Kronnie, Geertruy; Izraeli, Shai; Harris, Marian; Stevenson, Kristen E.; Neuberg, Donna; Silverman, Lewis B.; Sallan, Stephen E.; Bradner, James E.; Hahn, William C.; Crispino, John D.; Pellman, David; Weinstock, David M. (2014)
      Down syndrome confers a 20-fold increased risk of B cell acute lymphoblastic leukemia (B-ALL)1 and polysomy 21 is the most frequent somatic aneuploidy amongst all B-ALLs2. Yet, the mechanistic links between chr.21 triplication ...
    • The use of small molecules in somatic-cell reprogramming 

      Federation, Alexander J; Bradner, James Elliott; Meissner, Alexander (Elsevier BV, 2014)
      Pioneering work over the past years has highlighted the remarkable ability of manipulating cell states through exogenous, mostly transcription factor-induced reprogramming. The use of small molecules and reprogramming by ...