Results 101 to 110 of about 33,428 (239)

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

Nature, 2016
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.
Shaokun Shu, Charles Y. Lin, H. He, R. Witwicki, D. Tabassum, Justin M. Roberts, M. Janiszewska, S. Huh, Yi Liang, J. Ryan, Ernest Doherty, Hisham Mohammed, Hao Guo, D. Stover, Muhammad B Ekram, Guillermo Peluffo, Jonathan D. Brown, C. D’Santos, I. Krop, D. Dillon, Michael R Mckeown, Christopher J. Ott, J. Qi, M. Ni, Prakash K. Rao, Melissa Duarte, Shwu-Yuan Wu, C. Chiang, L. Anders, R. Young, E. Winer, A. Letai, W. Barry, J. Carroll, Henry W. Long, Myles A. Brown, X. Liu, Clifford A. Meyer, J. Bradner, K. Polyak   +39 more
semanticscholar   +1 more source

Effect of Bromodomain and Extraterminal Inhibitors with Different Bromodomain Selectivity on Mesenchymal Stem Cells

International audienceAbstract This study examines the influence of bromodomain and extraterminal (BET) inhibitors with different selectivity for bromodomains on human mesenchymal stem cells (hMSCs).
Ebara, Mitsuhiro, Uto, Koichiro, Wong, Yung-Sing, Tanimoto, Riho   +3 more
core   +1 more source

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain

, 2018
The bromodomain and extra-terminal domain (BET) family of proteins bind acetylated lysine residues on histone proteins. The four BET bromodomainsBRD2, BRD3, BRD4, and BRDTeach contain two bromodomain modules.
Chun-wa Chung (1343454), David J. Hirst (1399282), Paul Bamborough (1343466), Emmanuel H. Demont (1399288), Matthew Lindon (1355946), Robert P. Law (2613493), Rab K. Prinjha (449759), Allan J. B. Watson (1369614), Stephen J. Atkinson (1297362), Laurie J. Gordon (1343442)   +9 more
core   +2 more sources

Humanized Candida and NanoBiT Assays Expedite Discovery of Bdf1 Bromodomain Inhibitors With Antifungal Potential

Advanced Science
The fungal Bromodomain and Extra‐Terminal (BET) protein Bdf1 is a potential antifungal target against invasive fungal infections. However, the need to selectively inhibit both Bdf1 bromodomains (BDs) over human orthologs and the lack of molecular tools ...
Kaiyao Wei, Marie Arlotto, Justin M. Overhulse, Tuan‐Anh Dinh, Yingsheng Zhou, Nathan J. Dupper, Jiayi Yang, Boris A. Kashemirov, Hasan Dawi, Cécile Garnaud, Gaëlle Bourgine, Flore Mietton, Morgane Champleboux, Amédé Larabi, Yordan Hayat, Rose‐Laure Indorato, Marjolaine Noirclerc‐Savoye, Dimitrios Skoufias, Muriel Cornet, Gwenaël Rabut, Charles E. McKenna, Carlo Petosa, Jérôme Govin   +22 more
doaj   +1 more source

Bromodomains: pockets with therapeutic potential

Trends in Molecular Medicine, 2014
Intense interest in the complex biology of the bromodomain (BRD) protein modules has fueled the development of novel small molecule inhibitors that target the acetyl-lysine (KAc) binding pocket of the BRD. BRD inhibition has revealed exciting opportunities for treating a variety of maladies such as cancer, inflammation, obesity, cardiovascular disease,
Papavassiliou, Kostas A., Papavassiliou, Athanasios G.   +1 more
openaire   +3 more sources

High affinity binding of H3K14ac through collaboration of bromodomains 2, 4 and 5 is critical for the molecular and tumor suppressor functions of PBRM1

Molecular Oncology, 2019
Polybromo‐1 (PBRM1) is an important tumor suppressor in kidney cancer. It contains six tandem bromodomains (BDs), which are specialized structures that recognize acetyl‐lysine residues.
Lili Liao, Nilda L. Alicea‐Velázquez, Lauren Langbein, Xiaohua Niu, Weijia Cai, Eun‐Ah Cho, Meiling Zhang, Celeste B. Greer, Qin Yan, Michael S. Cosgrove, Haifeng Yang   +10 more
doaj   +1 more source

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Journal of Medicinal Chemistry, 2017
The bromodomain and extra-terminal (BET) family proteins, consisting of BRD2, BRD3, BRD4, and testis-specific BRDT members, are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are considered to be attractive
Bing Zhou, Jiantao Hu, Fuming Xu, Zhuo Chen, Longchuan Bai, E. Fernández-Salas, Mei Lin, Liu Liu, Chao-Yie Yang, Yujun Zhao, D. McEachern, S. Przybranowski, Bo Wen, Duxin Sun, Shaomeng Wang   +14 more
semanticscholar   +1 more source

BET Bromodomain Inhibition of MYC-Amplified Medulloblastoma [PDF]

, 2014
PurposeMYC-amplified medulloblastomas are highly lethal tumors. Bromodomain and extraterminal (BET) bromodomain inhibition has recently been shown to suppress MYC-associated transcriptional activity in other cancers.
Weiss, William A.,, Cho, Yoon-Jae, Swartling, Fredrik J, Bolin, Sara,, Cheshier, Samuel H., Paolella, Brenton R., Wechsler-Reya, Robert, Zeid, Rhamy, Gibson, William J, Bandopadhayay, Pratiti,, Kieran, Mark W., Bradner, James E, Bradner, James E.,, Gibson, William J., Bolin, Sara, Cheshier, Samuel H, Liu, Kun-Wei, Schumacher, Steven E., Bergthold, Guillaume,, Cho, Yoon-Jae,, Beroukhim, Rameen,, Mitra, Siddhartha S., Weiss, William A, Nguyen, Brian, Beroukhim, Rameen, Schubert, Simone, Bandopadhayay, Pratiti, Schumacher, Steven E, Mitra, Siddhartha S, Gholamin, Sharareh, Bergthold, Guillaume, Yu, Furong, Qi, Jun, Tang, Yujie, Paolella, Brenton R, Vue, Nujsaubnusi, Kieran, Mark W, Masoud, Sabran, Swartling, Fredrik J.,   +38 more
core   +1 more source

Advancements in the development of non-BET bromodomain chemical probes [PDF]

, 2019
The bromodomain and extra terminal (BET) family of bromodomain‐containing proteins (BCPs) have been the subject of extensive research over the past decade, resulting in a plethora of high‐quality chemical probes for their tandem bromodomains.
Tomkinson, Nicholas C. O., Prinjhal, Rab K., Philip G. Humphreys, Clegg, Michael A., Michael A. Clegg, Nicholas C. O. Tomkinson, Humphreys, Philip G., Rab K. Prinjha   +7 more
core   +1 more source

Small molecule ligands of the BET-like bromodomain, SmBRD3, affect Schistosoma mansoni survival, oviposition, and development

, 2023
Schistosomiasis is a disease affecting over 200 million people worldwide, but its treatment relies on a single agent, praziquantel. To investigate new avenues for schistosomiasis control, we have conducted the first systematic analysis of bromodomain ...
Helen, Whiteland, Karl, Hoffmann, Josephine, Forde-Thomas, Manfred, Beckmann, Stuart, Conway, Anthony, Chan, Michael, McDonough, Rosa, Cookson, Darius, McArdle, Gilda, Padalino, Matthias, Schiedel   +10 more
core   +1 more source