Results 11 to 20 of about 12,390,722 (231)

Probing BRD Inhibition Substituent Effects in Bulky Analogues of (+)‐JQ1 [PDF]

Helvetica Chimica Acta, 2021
AbstractA series of bulky organometallic and organic analogues of the bromodomain (BRD) inhibitor (+)‐JQ1 have been prepared. The most potent, N‐[(adamantan‐1‐yl)methyl]‐2‐[(9S)‐7‐(4‐chlorophenyl)‐4,5,13‐trimethyl‐3‐thia‐1,8,11,12‐tetraazatricyclo[8.3.0.02,6]trideca‐2(6),4,7,10,12‐pentaen‐9‐yl]acetamide, 2e, showed excellent potency with an KD=ca.
Hassell‐Hart, Storm, Picaud, Sarah, Lengacher, Raphael, Csucker, Joshua, Millet, Regis, Gasser, Gilles, Alberto, Roger, Maple, Hannah, Felix, Robert, Leśnikowski, Zbigniew J, Stewart, Helen J S, Chevassut, Timothy J, Morley, Simon, Filippakopoulos, Panagis, Spencer, John   +14 more
openaire   +4 more sources

BET Inhibitor JQ1 Blocks Inflammation and Bone Destruction [PDF]

Journal of Dental Research, 2014
BET proteins are a group of epigenetic regulators controlling transcription through reading acetylated histone tails and recruiting transcription complexes. They are considered as potential therapeutic targets in many distinct diseases. A novel synthetic bromodomain and extraterminal domain (BET) inhibitor, JQ1, was proved to suppress oncogene ...
S, Meng, L, Zhang, Y, Tang, Q, Tu, L, Zheng, L, Yu, D, Murray, J, Cheng, S H, Kim, X, Zhou, J, Chen   +10 more
openaire   +2 more sources

Bromodomain inhibitor JQ1 reversibly blocks IFN-γ production [PDF]

Scientific Reports, 2019
AbstractAs a class, ‘BET’ inhibitors disrupt binding of bromodomain and extra-terminal motif (BET) proteins, BRD2, BRD3, BRD4 and BRDT, to acetylated histones preventing recruitment of RNA polymerase 2 to enhancers and promoters, especially super-enhancers, to inhibit gene transcription.
Gibbons, Hunter R., Mi, Deborah J., Farley, Virginia M., Esmond, Tashawna, Kaood, Mary B., Aune, Thomas M.   +5 more
openaire   +2 more sources

General mechanism of JQ1 in inhibiting various types of cancer

Molecular Medicine Reports, 2020
Bromodomain‑containing 4 (BRD4) is a histone modification reader and transcriptional regulator that has been reported to interact with acetylated lysine histone motifs transcription factors (TFs), transcription co‑activators and RNA polymerase II. The selective small molecule inhibitor JQ1, which binds competitively to bromodomains, has been reported ...
Jiang, Guojuan, Deng, Wanglong, Liu, Yang, Wang, Chengde   +3 more
openaire   +3 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

JQ1 is a potential therapeutic option for COPD patients with agrin overexpression [PDF]

American Journal of Physiology-Lung Cellular and Molecular Physiology, 2018
Chronic obstructive pulmonary disease (COPD) is one of the leading causes of morbidity and death worldwide. It is characterized by chronic pulmonary inflammation and obstructed airflow from the lungs. To date, there is no effective treatment for COPD. The activation of the agrin (AGRN-YAP pathway can promote heart regeneration. Because agrin can induce
Zhen, Xiao, Jing, Shu, Feng, Zhou, Yong, Han   +3 more
openaire   +2 more sources

Modulation of Virulence-Associated Traits in Aspergillus fumigatus by BET Inhibitor JQ1

Microorganisms, 2022
Aspergillus fumigatus is a disease-causing, opportunistic fungus that can establish infection due to its capacity to respond to a wide range of environmental conditions. Secreted proteins and metabolites, which play a critical role in fungal–host interactions and pathogenesis, are modulated by epigenetic players, such as bromodomain and extraterminal ...
Orekhova, Anastasia, De Angelis, Marta, Cacciotti, Andrea, Reverberi, Massimo, Rotili, Dante, Giorgi, Alessandra, Protto, Virginia, Bonincontro, Graziana, Fiorentino, Francesco, Zgoda, Victor, Mai, Antonello, Palamara, Anna Teresa, Simonetti, Giovanna   +12 more
openaire   +5 more sources

Metformin and JQ1 synergistically inhibit obesity-activated thyroid cancer [PDF]

Endocrine-Related Cancer, 2018
Compelling epidemiological evidence shows a strong positive correlation of obesity with thyroid cancer. In vivo studies have provided molecular evidence that high-fat-diet-induced obesity promotes thyroid cancer progression by aberrantly activating leptin-JAK2-STAT3 signaling in a mouse model
Sunmi, Park, Mark C, Willingham, Jun, Qi, Sheue-Yann, Cheng   +3 more
openaire   +2 more sources

Co-Encapsulation of Paclitaxel and JQ1 in Zein Nanoparticles as Potential Innovative Nanomedicine

Micromachines, 2022
The manuscript describes the development of zein nanoparticles containing paclitaxel (PTX) and the bromo-and extra-terminal domain inhibitor (S)-tertbutyl2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno(3,2-f)(1,2,4)triazolo(4,3-a)(1,4)diazepin-6-yl)acetate (JQ1) together with their cytotoxicity on triple-negative breast cancer cells.
Marilena Celano, Agnese Gagliardi, Valentina Maggisano, Nicola Ambrosio, Stefania Bulotta, Massimo Fresta, Diego Russo, Donato Cosco   +7 more
openaire   +3 more sources

JQ1 attenuates neuroinflammation by inhibiting the inflammasome-dependent canonical pyroptosis pathway in SAE [PDF]

Brain Research Bulletin, 2022
Abstract Sepsis-associated encephalopathy (SAE) manifests clinically in hyperneuroinflammation. Pyroptosis, which can induce an inflammatory cascade response, has been considered to be a causative factor of SAE. Evidence has shown that the bromo- and extraterminal (BET) proteins (including BRD2, BRD3, BRD4 and BRDT) inhibitor JQ1 can inhibit ...
Xiaolin Zhong, Zuyao Chen, Yajuan Wang, Mingli Mao, Yingcheng Deng, Mengmeng Shi, Yang Xu, Ling Chen, Wenyu Cao   +8 more
openaire   +2 more sources