Results 101 to 110 of about 37,262 (190)

Selective small molecule induced degradation of the BET bromodomain protein BRD4 [PDF]

, 2015
The Bromo- and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET selective bromodomain inhibitor JQ1.
Alessio Ciulli, Anders L., Baratta M. G., Baud M. G. J., Belkina A. C., Boi M., Brand M., Bretones G., Cheng Z., Chung C.-W., Corson T. W., Cyrus K., Delmore J. E., Filippakopoulos P., Filippakopoulos P., Filippakopoulos P., Galdeano C., Gallenkamp D., Gosmini R., Hnilicová J., Hon W.-C., Khan Y. M., Kwok-Ho Chan, Lamoureux F., Lee H., Li Z., McLure K. G., Mertz J. A., Michael Zengerle, Mirguet O., Nicodeme E., Prinjha R. K., Raina K., Sakamoto K. M., Sakamoto K. M., Schneekloth J. S., Seoane J., Shi J., Strasser A., Zuber J.   +39 more
core   +5 more sources

Response and resistance to BET bromodomain inhibitors in triple-negative breast cancer [PDF]

, 2014
Triple-negative breast cancer (TNBC) is a heterogeneous and clinically aggressive disease for which there is no targeted therapy. BET bromodomain inhibitors, which have shown efficacy in several models of cancer have not been evaluated in TNBC.
Anders, Lars, Barry, William T., Bradner, James, Brown, Jonathan, Brown, Myles, Carroll, Jason S., Chiang, Cheng-Ming, Dillon, Deborah, Doherty, Ernest, Duarte, Melissa, D’Santos, Clive, Ekram, Muhammad B., Guo, Hao, He, Housheng Hansen, Janiszewska, Michalina, Jin Huh, Sung, Krop, Ian E., Letai, Antony, Liang, Yi, Lin, Charles Y., Liu, X. Shirley, Long, Henry W., McKeown, Michael, Meyer, Clifford A., Mohammed, Hisham, Ni, Min, Ott, Christopher, Peluffo, Guillermo, Polyak, Kornelia, Qi, Jun, Rao, Prakash K., Roberts, Justin M., Ryan, Jeremy, Shu, Shaokun, Stover, Daniel G., Tabassum, Doris P., Winer, Eric P., Witwicki, Robert M., Wu, Shwu-Yuan, Young, Richard A.   +39 more
core   +1 more source

Bromodomains on the brain [PDF]

Science-Business eXchange, 2013
A Dana-Farber–led team has found that MYCN amplification provides a marker for sensitivity to BET bromodomain inhibition in neuroblastomas. GSK is using the marker as one criterion to select patients for a Phase I trial of its BET bromodomain inhibitor in cancer.
openaire   +1 more source

A novel carboxamide bromodomain inhibitor attenuates osteoarthritis via epigenetic repression of NF-κB and MAPK signaling

Frontiers in Immunology
Bromodomains are epigenetic readers that modulate gene expression linked to inflammation and cartilage degeneration. Emerging evidence suggests their dysregulation plays a pivotal role in osteoarthritis (OA) pathogenesis, making them promising ...
Hyemi Lee, Seong Jae Han, Subin Ok, Kwang Min Lee, Seungseok Choi, Injoo Yoon, Somang Choi, Jina Kim, Serim Ryu, Min-Hee Son, In-Hyun Lee, Chanmi Cho, Siyoung Yang   +12 more
doaj   +1 more source

BRD4 (bromodomain containing 4) [PDF]

Atlas of Genetics and Cytogenetics in Oncology and Haematology, 2011
Review on BRD4 (bromodomain containing 4), with data on DNA, on the protein encoded, and where the gene is implicated.
openaire   +1 more source

Identification of Novel Bromodomain-Containing Protein 4 (BRD4) Binders through 3D Pharmacophore-Based Repositioning Screening Campaign

Molecules
A 3D structure-based pharmacophore model built for bromodomain-containing protein 4 (BRD4) is reported here, specifically developed for investigating and identifying the key structural features of the (+)-JQ1 known inhibitor within the BRD4 binding site.
Ester Colarusso, Erica Gazzillo, Eleonora Boccia, Stefania Terracciano, Ines Bruno, Giuseppe Bifulco, Maria Giovanna Chini, Gianluigi Lauro   +7 more
doaj   +1 more source

Bromodomain and extra-terminal domain inhibition modulates the expression of pathologically relevant microRNAs in diffuse large B-cell lymphoma

Haematologica, 2018
Aberrant changes in microRNA expression contribute to lymphomagenesis. Bromodomain and extra-terminal domain inhibitors such as OTX015 (MK-8628, birabresib) have demonstrated preclinical and clinical activity in hematologic tumors.
Afua A. Mensah, Luciano Cascione, Eugenio Gaudio, Chiara Tarantelli, Riccardo Bomben, Elena Bernasconi, Domenico Zito, Andrea Lampis, Jens C. Hahne, Andrea Rinaldi, Anastasios Stathis, Emanuele Zucca, Ivo Kwee, Valter Gattei, Nicola Valeri, Maria E Riveiro, Francesco Bertoni   +16 more
doaj   +1 more source

Non-canonical reader modules of BAZ1A promote recovery from DNA damage

Nature Communications, 2017
ISWI chromatin remodelers regulate DNA accessibility and have been implicated in DNA damage repair. Here, the authors uncover functions, in response to DNA damage, for the bromodomain of the ISWI subunit BAZ1B and for the non-canonical PHD and ...
Mariano Oppikofer, Meredith Sagolla, Benjamin Haley, Hui-Min Zhang, Sarah K. Kummerfeld, Jawahar Sudhamsu, E. Megan Flynn, Tianyi Bai, Jennifer Zhang, Claudio Ciferri, Andrea G. Cochran   +10 more
doaj   +1 more source

The Histone Deacetylase SIRT6 Restrains Transcription Elongation via Promoter-Proximal Pausing. [PDF]

, 2019
Transcriptional regulation in eukaryotes occurs at promoter-proximal regions wherein transcriptionally engaged RNA polymerase II (Pol II) pauses before proceeding toward productive elongation.
Ablondi, Eileen, Adelman, Karen, Chang, Andrew, Choi, Jee-Eun, Etchegaray, Jean-Pierre, Ferrer, Christina, Goren, Alon, Henriques, Telmo, Ji, Fei, Li, Catherine, Mostoslavsky, Raul, Nakadai, Tomoyoshi, Nechaev, Sergei, Ramaswamy, Sridhar, Roeder, Robert G, Ross, Kenneth N, Sadreyev, Ruslan I, Samarakkody, Ann, Van Rechem, Capucine, Whetstine, Johnathan R, Zhong, Lei   +20 more
core   +1 more source

Bromodomain Protein Inhibition Protects β-Cells from Cytokine-Induced Death and Dysfunction via Antagonism of NF-κB Pathway

Cells
Cytokine-induced β-cell apoptosis is a major pathogenic mechanism in type 1 diabetes (T1D). Despite significant advances in understanding its underlying mechanisms, few drugs have been translated to protect β-cells in T1D.
Vinny Negi, Jeongkyung Lee, Varun Mandi, Joseph Danvers, Ruya Liu, Eliana M. Perez-Garcia, Feng Li, Rajaganapati Jagannathan, Ping Yang, Domenic Filingeri, Amit Kumar, Ke Ma, Mousumi Moulik, Vijay K. Yechoor   +13 more
doaj   +1 more source