Results 31 to 40 of about 14,237 (205)

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 vivostudies 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 of thyroid cancer (ThrbPV/PVPten+/−mice).
Sunmi, Park, Mark C, Willingham, Jun, Qi, Sheue-Yann, Cheng   +3 more
openaire   +2 more sources

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

The BRD4 inhibitor JQ1 suppresses tumor growth by reducing c-Myc expression in endometrial cancer

Journal of Translational Medicine, 2022
Background Endometrial cancer (EC) is the most common gynecological malignancy in developed countries. Efficacy of the bromodomain 4 (BRD4) inhibitor JQ1 has been reported for the treatment of various human cancers, but its potential impact on EC remains
Yingxin Pang, Gaigai Bai, Jing Zhao, Xuan Wei, Rui Li, Jie Li, Shunxue Hu, Lu Peng, Peishu Liu, Hongluan Mao   +9 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

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

BRD4 promotes heterotopic ossification through upregulation of LncRNA MANCR

Bone & Joint Research, 2021
Aims: Acquired heterotopic ossification (HO) is a debilitating disease characterized by abnormal extraskeletal bone formation within soft-tissues after injury. The exact pathogenesis of HO remains unknown.
Lei Liu, ZiHao Li, Siwen Chen, Haowen Cui, Xiang Li, Guo Dai, Fangling Zhong, Wenjun Hao, Kuibo Zhang, Hui Liu   +9 more
doaj   +1 more source

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

The BET Protein Inhibitor JQ1 Decreases Hypoxia and Improves the Therapeutic Benefit of Anti-PD-1 in a High-Risk Neuroblastoma Mouse Model

Cells, 2022
Anti-programmed death 1 (PD-1) is a revolutionary treatment for many cancers. The response to anti-PD-1 relies on several properties of tumor and immune cells, including the expression of PD-L1 and PD-1.
Delphine Sauvage, Manon Bosseler, Elodie Viry, Georgia Kanli, Anais Oudin, Guy Berchem, Olivier Keunen, Bassam Janji   +7 more
doaj   +1 more source

Inhibition of Brd4 by JQ1 Promotes Functional Recovery From Spinal Cord Injury by Activating Autophagy

Frontiers in Cellular Neuroscience, 2020
Spinal cord injury (SCI) is a destructive neurological disorder that is characterized by impaired sensory and motor function. Inhibition of bromodomain protein 4 (Brd4) has been shown to promote the maintenance of cell homeostasis by activating autophagy.
Yao Li, Jie Xiang, Jing Zhang, Jiahao Lin, Yaosen Wu, Xiangyang Wang   +5 more
doaj   +1 more source