Results 41 to 50 of about 20,657 (229)

BET Bromodomain Blockade Mitigates Intimal Hyperplasia in Rat Carotid Arteries

EBioMedicine, 2015
Background: Intimal hyperplasia is a common cause of many vasculopathies. There has been a recent surge of interest in the bromo and extra-terminal (BET) epigenetic “readers” including BRD4 since the serendipitous discovery of JQ1(+), an inhibitor ...
Bowen Wang, Mengxue Zhang, Toshio Takayama, Xudong Shi, Drew Alan Roenneburg, K. Craig Kent, Lian-Wang Guo   +6 more
doaj   +1 more source

Mammary molecular portraits reveal lineage-specific features and progenitor cell vulnerabilities. [PDF]

, 2018
The mammary epithelium depends on specific lineages and their stem and progenitor function to accommodate hormone-triggered physiological demands in the adult female.
Abe, Akalin, Alison E. Casey, Ankit Sinha, Asselin-Labat, Buenrostro, Cardiff, Cerami, Cheryl Arrowsmith, Chlebowski, Cox, Cox, Dalia Barsyte-Lovejoy, Daniel De Carvalho, Deugnier, Dos Santos, Edgar, Eirew, Eirew, Eisen, Erik Drysdale, Gary Bader, Gascard, Genevieve Deblois, Gu, Hal Berman, Heinz, Hennighausen, Herschkowitz, Hu, Hui Fang, Huston, Hyeyeon Kim, Ignatchenko, Jackson, Jennifer Cruickshank, Joshi, Joshi, Joshi, Julie Livingstone, Kaltenborn, Kauff, Kelsey, Kendrick, Kiechl, Kislinger, Koboldt, Kotsopoulos, Krueger, Kucera, Labarge, Li, Lim, Lim, Lin, Loenen, Lucas, Lydon, Marotti, Maruyama, Mathieu Lupien, McLean, Meissner, Merico, Michailidou, Michalak, Mohammed, Molyneux, Mona Shehata, Nguyen, Pal, Pathania, Paul C. Boutros, Paul Waterhouse, Pei, Pellacani, Pirashaanthy Tharmapalan, Rajat Singhania, Rama Khokha, Reimand, Rios, Rios, Rugg-Gunn, Ruth Isserlin, Schimanski, Shackleton, Shannon, Shehata, Shiah, Shu, Sigl, Smith, Smyth, Stefan Hofer, Stefan Knapp, Stingl, Storey, Stunnenberg, Subramanian, Swneke Bailey, Thomas Kislinger, Tiago Medina, Tomasetti, van Amerongen, Van Keymeulen, Van Keymeulen, Visvader, Wang, Wojtowicz, Wuidart, Yu-Jia Shiah, Zhang   +111 more
core   +2 more sources

JQ1 affects BRD2-dependent and independent transcription regulation without disrupting H4-hyperacetylated chromatin states

Epigenetics, 2018
The bromodomain and extra-terminal domain (BET) proteins are promising drug targets for cancer and immune diseases. However, BET inhibition effects have been studied more in the context of bromodomain-containing protein 4 (BRD4) than BRD2, and the BET ...
Lusy Handoko, Bogumil Kaczkowski, Chung-Chau Hon, Marina Lizio, Masatoshi Wakamori, Takayoshi Matsuda, Takuhiro Ito, Prashanti Jeyamohan, Yuko Sato, Kensaku Sakamoto, Shigeyuki Yokoyama, Hiroshi Kimura, Aki Minoda, Takashi Umehara   +13 more
doaj   +1 more source

Comprehensive exploration of JQ1 and GSK2801 targets in breast cancer using network pharmacology and molecular modeling approaches

Computational and Structural Biotechnology Journal, 2023
JQ1 and GSK2801 are bromo domain inhibitors (BDI) known to exhibit enhanced anti-cancer activity when combined with other agents. However, the underlying molecular mechanisms behind such enhanced activity remain unclear.
Nanda Kumar Yellapu, Dong Pei, Emily Nissen, Jeffrey A. Thompson, Devin C. Koestler   +4 more
doaj   +1 more source

Thermoelectric efficiency of three-terminal quantum thermal machines [PDF]

, 2014
The efficiency of a thermal engine working in linear response regime in a multi-terminals configuration is discussed. For the generic three-terminal case, we provide a general definition of local and non-local transport coefficients: electrical and ...
Benenti, Giuliano, Bosisio, Riccardo, Fazio, Rosario, Giovannetti, Vittorio, Mazza, Francesco, Taddei, Fabio   +5 more
core   +6 more sources

Open Access Could Transform Drug Discovery: A Case Study of JQ1 [PDF]

Expert Opinion on Drug Discovery, 2016
The cost to develop a new drug from target discovery to market is a staggering $1.8 billion, largely due to the very high attrition rate of drug candidates and the lengthy transition times during development. Open access is an emerging model of open innovation that places no restriction on the use of information and has the potential to accelerate the ...
Zeeshaan, Arshad, James, Smith, Mackenna, Roberts, Wen Hwa, Lee, Ben, Davies, Kim, Bure, Georg A, Hollander, Sue, Dopson, Chas, Bountra, David, Brindley   +9 more
openaire   +2 more sources

Synergistic inhibition of pancreatic cancer with anti-PD-L1 and c-Myc inhibitor JQ1

OncoImmunology, 2019
Human pancreatic ductal adenocarcinoma (PDAC) exhibits marginal responses to anti-PD-1/PD-L1 immunotherapy and its mechanism remains poorly understood. We have investigated the effect of anti-PD-L1 and c-Myc inhibition in PDAC.
Yu Pan, Qinglin Fei, Ping Xiong, Jianyang Yang, Zheyang Zhang, Xianchao Lin, Minggui Pan, Fengchun Lu, Heguang Huang   +8 more
doaj   +1 more source

Effect of bet missense mutations on bromodomain function, inhibitor binding and stability [PDF]

, 2016
Lysine acetylation is an important epigenetic mark regulating gene transcription and chromatin structure. Acetylated lysine residues are specifically recognized by bromodomains, small protein interaction modules that read these modification in a ...
Alessandra, Pasquo, Chiaraluce, Roberta, Consalvi, Valerio, Cynthia, Tallant, Lori, Clorinda, Lori, Laura, Petrosino, Maria, Stefan, Knapp   +7 more
core   +2 more sources

Scalable syntheses of the BET bromodomain inhibitor JQ1

Tetrahedron Letters, 2015
We have developed methods involving the use of alternate, safer reagents for the scalable syntheses of the potent BET bromodomain inhibitor JQ1. A one-pot three step method, involving the conversion of a benzodiazepine to a thioamde using Lawesson's reagent, followed by amidrazone formation and installation of the triazole moiety furnished JQ1.
Syeda, Shameem Sultana, Jakkaraj, Sudhakar, Georg, Gunda I.   +2 more
openaire   +2 more sources

BET inhibitor JQ1 enhances anti-tumor immunity and synergizes with PD-1 blockade in CRC

Journal of Cancer, 2022
Most colorectal cancer (CRC) patients are insensitive to immune checkpoint inhibitors (ICIs) due to the immunosuppressive tumor microenvironment (TME). Epigenetic factors such as the bromo-and extraterminal domain (BET) family proteins may be responsible
Huijin Wang, Guangyao Liu, Xinghan Jin, Shenglei Song, Songyao Chen, Peiqing Zhou, Huanhuan Li, Jianming Liang, Bo Li, Changhua Zhang, Yulong He   +10 more
semanticscholar   +1 more source