Results 11 to 20 of about 14,237 (205)

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

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

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 attenuated LPS-induced microglial inflammation via MAPK/NFκB signaling

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   +2 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

JQ1 suppresses tumor growth through downregulating LDHA in ovarian cancer*

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   +5 more sources

Transcriptome analysis of dominant-negative Brd4 mutants identifies Brd4-specific target genes of small molecule inhibitor JQ1 [PDF]

Scientific Reports, 2017
The bromodomain protein Brd4 is an epigenetic reader and plays a critical role in the development and maintenance of leukemia. Brd4 binds to acetylated histone tails and activates transcription by recruiting the positive elongation factor P-TEFb.
Tim-Michael Decker, Michael Kluge, Stefan Krebs, Nilay Shah, Helmut Blum, Caroline C. Friedel, Dirk Eick   +6 more
doaj   +2 more sources

(+)-JQ1 Upregulates SIRT3 to Suppress cGAS/STING Pathway-Mediated Neuronal Inflammation and Ferroptosis After Hypoxic-Ischemic Encephalopathy. [PDF]

Drug Des Devel Ther
Qianqian Yu,1,2,* Jiahao Ou,1,2,* Yuqi Luo,1,2,* Ming Shen,1,2 Jia Lou,3 Saizhi Jiang,4,5 Lizi Lin,5 Shutian Zhang,5 Jianghu Zhu,1,2 Zhenlang Lin,1,2 Mingchu Fang1,2 1Department of Neonatology, The Second Affiliated Hospital and ...
Yu Q, Ou J, Luo Y, Shen M, Lou J, Jiang S, Lin L, Zhang S, Zhu J, Lin Z, Fang M.   +10 more
europepmc   +2 more sources

A photothermal immune hydrogel dressing for enhanced post-melanoma resection treatment. [PDF]

J Nanobiotechnology
Postoperative complications such as tumor recurrence, wound infections, and delayed tissue regeneration persist as critical challenges in melanoma management.
Tan D, Zhu W, Liu S, Liao F, Xu X, Luo J, Zhang S, Xie Q, Liang Y, Yu Z, Zhang P.   +10 more
europepmc   +2 more sources

Arsenic sulfide combined with JQ1, chemotherapy agents, or celecoxib inhibit gastric and colon cancer cell growth

Drug Design, Development and Therapy, 2015
Lian Zhang,1 Yingying Tong,1 Xiuli Zhang,1 Minggui Pan,2,3 Siyu Chen1 1Department of Oncology, Xin Hua Hospital Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, People’s Republic of China; 2Department of Oncology and ...
Zhang L, Tong Y, Zhang X, Pan M, Chen S
doaj   +1 more source