Results 11 to 20 of about 13,555 (204)

The BET inhibitor JQ1 targets fat metabolism and counteracts obesity

Journal of Advanced Research
Introduction: Obesity, one of the most frequent health problems in the adult population, is a condition characterized by excessive white adipose tissue accumulation and accompanied by the increased risk to develop other disorders such as type II diabetes,
Claudia Fornelli, Alessia Sofia Cento, Lorenzo Nevi, Raffaella Mastrocola, Gustavo Ferreira Alves, Giuseppina Caretti, Massimo Collino, Fabio Penna   +7 more
doaj   +4 more sources

(+)-JQ1 attenuated LPS-induced microglial inflammation via MAPK/NFκB signaling [PDF]

Cell & Bioscience, 2018
Background Microglia activation is a crucial event in neurodegenerative disease. The depression of microglial inflammatory response is considered a promising therapeutic strategy.
Huanhuan Wang, Wenhai Huang, Meihao Liang, Yingying Shi, Chixiao Zhang, Qin Li, Meng Liu, Yikai Shou, Hongping Yin, Xiaozheng Zhu, Xiaoyan Sun, Yu Hu, Zhengrong Shen   +12 more
doaj   +4 more sources

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
core   +7 more sources

Scalable syntheses of the BET bromodomain inhibitor JQ1 [PDF]

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   +3 more sources

Impact of Short-Term (+)-JQ1 Exposure on Mouse Aorta: Unanticipated Inhibition of Smooth Muscle Contractility

Cells, 2023
(+)-JQ1, a specific chemical inhibitor of bromodomain and extraterminal (BET) family protein 4 (BRD4), has been reported to inhibit smooth muscle cell (SMC) proliferation and mouse neointima formation via BRD4 regulation and modulate endothelial nitric ...
Binjie Yan, Yu Gui, Yanan Guo, Jiaxing Sun, Mahmoud Saifeddine, Jingti Deng, Joseph A. Hill, Morley D. Hollenberg, Zhi-Sheng Jiang, Xi-Long Zheng   +9 more
doaj   +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   +3 more sources

JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer* [PDF]

Oncotarget, 2015
Amplification and overexpression of c-Myc is commonly seen in human ovarian cancers, and this could be a potentially novel therapeutic target for this disease. JQ1, a selective small-molecule BET bromodomain (BRDs) inhibitor, has been found to suppress tumor progression in several cancer cell types.
Haifeng, Qiu, Amanda L, Jackson, Joshua E, Kilgore, Yan, Zhong, Leo Li-Ying, Chan, Paola A, Gehrig, Chunxiao, Zhou, Victoria L, Bae-Jump   +7 more
openaire   +4 more sources

JQ1 attenuates psychostimulant- but not opioid-induced conditioned place preference

Behavioural Brain Research, 2022
Epigenetic mechanisms play important roles in the neurobiology of substance use disorder. In particular, bromodomain and extra-terminal domain (BET) proteins, a class of histone acetylation readers, have been found to regulate cocaine conditioned behaviors, but their role in the behavioral response to other drugs of abuse remains unclear.
C J, Babigian, H J, Wiedner, C, Wahlestedt, G C, Sartor   +3 more
openaire   +3 more sources

BET Protein Inhibitor JQ1 Modulates Mitochondrial Dysfunction and Oxidative Stress Induced by Chronic Kidney Disease

Antioxidants, 2023
Among the mechanisms involved in the progression of kidney disease, mitochondrial dysfunction has special relevance. Epigenetic drugs such as inhibitors of extra-terminal domain proteins (iBET) have shown beneficial effects in experimental kidney disease,
Sandra Rayego-Mateos, Pamela Basantes, José Luis Morgado-Pascual, Beatriz Brazal Prieto, Beatriz Suarez-Alvarez, Alberto Ortiz, Carlos Lopez-Larrea, Marta Ruiz-Ortega   +7 more
doaj   +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.
Anastasia Orekhova, Marta De Angelis, Andrea Cacciotti, Massimo Reverberi, Dante Rotili, Alessandra Giorgi, Virginia Protto, Graziana Bonincontro, Francesco Fiorentino, Victor Zgoda, Antonello Mai, Anna Teresa Palamara, Giovanna Simonetti   +12 more
doaj   +5 more sources