GSK-J4: An H3K27 histone demethylase inhibitor, as a potential anti-cancer agent.
Sign Up to like & getrecommendations! Published in 2023 at "International journal of cancer"
DOI: 10.1002/ijc.34559
Abstract: Aberrant epigenetic modifications are emerging as potent drivers of tumor initiation and progression. The deregulation of H3K27me3 marks has shown to play an important role in cancer progression in several cancers. The H3K27me3 mark is… read more here.
Keywords: demethylase inhibitor; cancer; anti cancer; histone demethylase ... See more keywords
Antiproliferative effect of the histone demethylase inhibitor GSK‐J4 in chondrosarcomas
Sign Up to like & getrecommendations! Published in 2019 at "IUBMB Life"
DOI: 10.1002/iub.2110
Abstract: Chondrosarcoma (CS) is the second most common malignant bone sarcoma. Its treatment remains an issue, because this tumor is radio‐ and chemo‐resistant. In the present study, we investigated the antitumoral potential of GSK‐J4, a small… read more here.
Keywords: demethylase; antiproliferative effect; cisplatin; proliferation ... See more keywords
Molecular docking study of GSK‐3β interaction with nomilin, kihadanin B, and related limonoids and triterpenes with a furyl‐δ‐lactone core
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Biochemical and Molecular Toxicology"
DOI: 10.1002/jbt.23130
Abstract: Glycogen synthase kinase‐3β (GSK‐3β) is a target enzyme considered for the treatment of multiple human diseases, from neurodegenerative pathologies to viral infections and cancers. Numerous inhibitors of GSK‐3β have been discovered but thus far only… read more here.
Keywords: furyl lactone; natural products; gsk; lactone core ... See more keywords
Jumonji domain containing-3 (JMJD3) inhibition attenuates IL-1β-induced chondrocytes damage in vitro and protects osteoarthritis cartilage in vivo
Sign Up to like & getrecommendations! Published in 2020 at "Inflammation Research"
DOI: 10.1007/s00011-020-01356-8
Abstract: Objectives This study aimed to explore the effects and relative mechanism of JMJD3 on knee osteoarthritis (OA). Methods In this study, we first analyzed the expression of JMJD3 in OA cartilage using western blot and… read more here.
Keywords: jmjd3; group; damage; vitro ... See more keywords
Therapeutic potential of GSK-J4, a histone demethylase KDM6B/JMJD3 inhibitor, for acute myeloid leukemia
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Cancer Research and Clinical Oncology"
DOI: 10.1007/s00432-018-2631-7
Abstract: PurposeAcute myeloid leukemia (AML) is a heterogeneous disease with poor outcomes. Despite increased evidence shows that dysregulation of histone modification contributes to AML, specific drugs targeting key histone modulators are not applied in the clinical… read more here.
Keywords: treatment; kdm6b; gsk; aml ... See more keywords
Receptor-based pharmacophore modeling, virtual screening, and molecular docking studies for the discovery of novel GSK-3β inhibitors
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Modeling"
DOI: 10.1007/s00894-019-4032-5
Abstract: AbstractConsidering the emerging importance of glycogen synthase kinase 3 beta (GSK-3β) inhibitors in treatment of Alzheimer’s disease, multi-protein structure receptor-based pharmacophore modeling was adopted to generate a 3D pharmacophore model for (GSK-3β) inhibitors. The generated… read more here.
Keywords: based pharmacophore; receptor based; molecular docking; pharmacophore modeling ... See more keywords
GSK-3β inhibition protects human nucleus pulposus cell against oxidative stress-inducing apoptosis through mitochondrial pathway.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular biology reports"
DOI: 10.1007/s11033-022-07218-2
Abstract: BACKGROUND Oxidative stress in the intervertebral disc leads to nucleus pulposus (NP) degeneration by inducing cell apoptosis. However, the molecular mechanisms underlying this process remain unclear. Increasing evidence indicates that GSK-3β is related to cell… read more here.
Keywords: apoptosis; inhibition; oxidative stress; gsk ... See more keywords
Inhibition of Noncanonical Ca2+ Oscillation/Calcineurin/GSK-3β Pathway Contributes to Anti-Inflammatory Effect of Sigma-1 Receptor Activation.
Sign Up to like & getrecommendations! Published in 2021 at "Neurochemical research"
DOI: 10.1007/s11064-021-03439-2
Abstract: Further understanding the mechanism for microglia activation is necessary for developing novel anti-inflammatory strategies. Our previous study found that the activation of sigma-1 receptor can effectively inhibit the neuroinflammation, independent of the canonical mechanisms, such… read more here.
Keywords: anti inflammatory; calcineurin; activation; sigma receptor ... See more keywords
Portraying the selectivity of GSK-3 inhibitors towards CDK-2 by 3D similarity and molecular docking
Sign Up to like & getrecommendations! Published in 2018 at "Structural Chemistry"
DOI: 10.1007/s11224-018-1224-z
Abstract: The striking structural resemblance between adenosine triphosphate (ATP) binding sites of glycogen synthase kinase-3 (GSK-3) and cyclin-dependent kinase-2 (CDK-2) raises numerous off-target selectivity problems in lead-identification processes that may jeopardize their progress into safe and… read more here.
Keywords: similarity; portraying selectivity; molecular docking; selectivity ... See more keywords
The antidepressant-like effect of guanosine is dependent on GSK-3β inhibition and activation of MAPK/ERK and Nrf2/heme oxygenase-1 signaling pathways
Sign Up to like & getrecommendations! Published in 2019 at "Purinergic Signalling"
DOI: 10.1007/s11302-019-09681-2
Abstract: Although guanosine is an endogenous nucleoside that displays antidepressant-like properties in several animal models, the mechanism underlying its antidepressant-like effects is not well characterized. The present study aimed at investigating the involvement of ERK/GSK-3β and… read more here.
Keywords: like effect; gsk; effect guanosine; antidepressant like ... See more keywords
Protective Effect of Morphine Against the Oxidant-Induced Injury in H9c2 Cells
Sign Up to like & getrecommendations! Published in 2018 at "Cardiovascular Toxicology"
DOI: 10.1007/s12012-018-9448-0
Abstract: There are some indications that morphine may exert myocardial protective effects under certain conditions. The aim of the present study was to investigate the effect of morphine on viability and oxidative state of H9c2 cells… read more here.
Keywords: morphine; h9c2 cells; effect morphine; gsk ... See more keywords