Results 41 to 50 of about 13,555 (204)
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 +8 more
openaire +2 more sources
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 +4 more
doaj +1 more source
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 +7 more
doaj +1 more source
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 +6 more
doaj +1 more source
Synergistic anti-proliferative activity of JQ1 and GSK2801 in triple-negative breast cancer
BMC Cancer, 2022 Background Triple-negative breast cancer (TNBC) constitutes 10–20% of breast cancers and is challenging to treat due to a lack of effective targeted therapies. Previous studies in TNBC cell lines showed in vitro growth inhibition when JQ1 or GSK2801 were
Nanda Kumar Yellapu +6 more
doaj +1 more source
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 +5 more
doaj +1 more source
Journal of Nanobiotechnology, 2022 Although combination chemoimmunotherapy shows promising clinical results for cancer treatment, this approach is largely restricted by variable objective response rate and severe systemic adverse effects of immunotherapeutic antibody and chemotherapeutic ...
Jun Gu +9 more
doaj +1 more source
Angewandte Chemie, EarlyView.Click‐to‐release (C2R) chemistry is redirected from payload liberation toward ligand‐directed covalent protein labeling through a transient dihydropyridazine methide (DHP‐methide). This concept opens the way to dual‐functional systems combining covalent target engagement with controlled effector release.
Dóra Kern +9 more
wiley +2 more sources
VDAC1 is regulated by BRD4 and contributes to JQ1 resistance in breast cancer
Oncology Letters, 2019 Voltage-dependent anion channels (VDACs) are situated in the outer membrane of the mitochondria and serve as gatekeepers that control metabolite and ion exchange between the cytosol and mitochondria. VDAC1 is one of the most studied members of the VDAC protein family and is overexpressed in multiple types of cancer.
Yang, Guochao +7 more
openaire +3 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 ...
Arshad Z +9 more
openaire +3 more sources