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https://www.readbyqxmd.com/read/29435775/quercetin-prevents-in-vivo-and-in-vitro-myocardial-hypertrophy-through-the-proteasome-gsk-3-pathway
#1
Kuixiang Chen, Mubarak Rekep, Wei Wei, Qian Wu, Qin Xue, Sujuan Li, Jiahui Tian, Quan Yi, Genshui Zhang, Guiping Zhang, Qing Xiao, Jiandong Luo, Yinghua Liu
PURPOSE: Quercetin, a flavonoid, has been reported to ameliorate cardiovascular diseases, such as cardiac hypertrophy. However, the mechanism is not completely understood. In this study, a mechanism related to proteasome-glycogen synthesis kinase 3 (GSK-3) was elucidated in rats and primary neonatal cardiomyocytes. METHODS: Rats were subjected to sham or constriction of abdominal aorta surgery groups and treated with or without quercetin for 8 weeks. Angiotensin II (Ang II)-induced primary cardiomyocytes were cultured with quercetin treatment or not for 48 h...
February 12, 2018: Cardiovascular Drugs and Therapy
https://www.readbyqxmd.com/read/29433844/glycogen-synthase-kinase-3%C3%AE-activity-and-cognitive-functioning-in-patients-with-bipolar-i-disorder
#2
Klaus Munkholm, Kamilla Woznica Miskowiak, Anne Sophie Jacoby, Maj Vinberg, Leda Leme Talib, Wagner Farid Gattaz, Lars Vedel Kessing
Cognitive deficits are common in patients with bipolar disorder (BD) in remission and may be associated with glycogen synthase kinase-3 (GSK-3) activity, which is inhibited by lithium. GSK-3 may be a relevant treatment target for interventions tailored at cognitive disturbances in BD but the relation between GSK-3 activity, cognition and lithium treatment is unknown. We therefore investigated the possible association between GSK-3 activity and cognition and whether lithium treatment moderates this association in patients with BD...
February 9, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29400073/oral-hormonal-therapy-with-ethinylestradiol-levonorgestrel-improves-insulin-resistance-obesity-and-glycogen-synthase-kinase-3-independent-of-circulating-mineralocorticoid-in-estrogen-deficient-rats
#3
Oluwaseun Aremu Adeyanju, Olaniyi Soetan, Ayodele Soladoye, Lawrence A Aderemi Olatunji
Estrogen deficiency has been associated with increased cardiovascular diseases (CVD) and recent clinical trials of standard formulations of hormonal therapies have not demonstrated consistent beneficial effects. Estrogen-progestin therapy has been used as exogenous estrogen to normalise depressed estrogen level during menopause. Ovariectomized rodents mimic estrogen-deficient state in that they develop cardiometabolic dysfunction, including insulin resistance (IR).We therefore hypothesized that hormonal therapy with combined oral contraceptive steroids, ethinylestradiol/levonorgestrel (EEL) improves IR, obesity and glycogen synthase kinase-3 (GSK-3) through reduction in circulating mineralocorticoid level in ovariectomized rats...
February 3, 2018: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/29396901/fine-tuning-of-canonical-wnt-stimulation-enhances-differentiation-of-pluripotent-stem-cells-independent-of-%C3%AE-catenin-mediated-t-cell-factor-signaling
#4
Joseph Chen, Christian M Nefzger, Fernando J Rossello, Yu B Y Sun, Sue Mei Lim, Xiaodong Liu, Suzan de Boer, Anja S Knaupp, Jinhua Li, Kathryn C Davidson, Jose M Polo, Tiziano Barberi
The canonical Wnt/β-catenin pathway is crucial for early embryonic patterning, tissue homeostasis, and regeneration. While canonical Wnt/β-catenin stimulation has been used extensively to modulate pluripotency and differentiation of pluripotent stem cells (PSCs), the mechanism of these two seemingly opposing roles has not been fully characterized and is currently largely attributed to activation of nuclear Wnt target genes. Here, we show that low levels of Wnt stimulation via ectopic expression of Wnt1 or administration of glycogen synthase kinase-3 inhibitor CHIR99021 significantly increases PSC differentiation into neurons, cardiomyocytes and early endodermal intermediates...
February 2, 2018: Stem Cells
https://www.readbyqxmd.com/read/29388174/gsk-3-inhibitors-a-double-edged-sword-an-update-on-tideglusib
#5
Theodore Lemuel Mathuram, Lisa M Reece, Kotturathu Mammen Cherian
GSK-3 inhibitors are an emerging tool for clinical interventions in human diseases and represent a niche area in combinational therapy. They possess diverse facets in applications of nervous system disorders, Type 2 diabetes, regenerative medicine and cancer. However, conflicting reports suggest the controversial role of GSK-3 inhibitors in cancers. This review aims to highlight the rise of GSK-3 inhibitors as tools for molecular-targeted research and its shift to a promising drug candidate. The review also focuses on key GSK-3 inhibitors and their roles in cancer and regenerative medicine with special emphasis to tideglusib...
January 31, 2018: Drug Research
https://www.readbyqxmd.com/read/29382566/overexpression-of-the-14-3-3%C3%AE-protein-in-uterine-leiomyoma-cells-results-in-growth-retardation-and-increased-apoptosis
#6
Qi Shen, Xiaoli Hu, Lulu Zhou, Shuangwei Zou, Lu-Zhe Sun, Xueqiong Zhu
Protein 14-3-3γ was significantly reduced in human uterine leiomyoma compared to the adjacent normal myometrium tissue. To investigate the possible link between the reduced 14-3-3γ expression and uterine leiomyoma growth, we have overexpressed 14-3-3γ protein in uterine leiomyomal cells and its effects on cell proliferation and apoptosis were analyzed. Over-expression of 14-3-3γ was achieved by transducing into two types of uterine leiomyoma cells (primary culture cells and immortal stem cells) with a 14-3-3γ expressing adenovirus vector...
January 27, 2018: Cellular Signalling
https://www.readbyqxmd.com/read/29335245/cdk9-mediated-phosphorylation-controls-the-interaction-of-tip60-with-the-transcriptional-machinery
#7
Prisca Brauns-Schubert, Florian Schubert, Manuela Wissler, Martina Weiss, Lisa Schlicher, Simon Bessler, Mariam Safavi, Cornelius Miething, Christoph Borner, Tilman Brummer, Ulrich Maurer
The acetyltransferase TIP60 is regulated by phosphorylation, and we have previously shown that phosphorylation of TIP60 on S86 by GSK-3 promotes p53-mediated induction of the BCL-2 protein PUMA. TIP60 phosphorylation by GSK-3 requires a priming phosphorylation on S90, and here, we identify CDK9 as a TIP60S90 kinase. We demonstrate that a phosphorylation-deficient mutant, TIP60S90A, exhibits reduced interaction with chromatin, histone 3 and RNA Pol II, while its association with the TIP60 complex subunit EPC1 is not affected...
January 15, 2018: EMBO Reports
https://www.readbyqxmd.com/read/29334667/lithium-a-classic-drug-in-psychiatry-improves-nilotinib-mediated-antileukemic-effects
#8
Janaína Peixoto-da-Silva, Andrana K Calgarotto, Katiucha R Rocha, Caroline Palmeira-Dos-Santos, Soraya S Smaili, Gustavo J S Pereira, Fernando V Pericole, Adriana da Silva S Duarte, Sara T O Saad, Claudia Bincoletto
Although Tyrosine kinase inhibitors (TKIs) that target Bcr-Abl play a key role in Chronic Myeloid Leukemia (CML) therapy, they do not eradicate CML-initiating cells, which lead to the emergence of drug resistance. Here we used the lithium, a GSK-3 inhibitor, to attempt to potentiate the effects of nilotinib against leukemia cells. For this purpose, a K562 leukemia cell line and bone marrow cells from untreated Chronic Myeloid Leukemia (CML) patients, prior to any exposure to TKIs, were used as a model. Our results demonstrated that the combination of lithium + nilotinib (L + N) induced K562-cell death and cleaved caspase-3 when compared to lithium or nilotinib alone, accompanied by GSK-3β phosphorylation and Bcr-Abl oncoprotein levels reduction...
January 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29310812/pgbr-extract-ameliorates-tnf-%C3%AE-induced-insulin-resistance-in-hepatocytes
#9
Fu-Chih Chen, Kuo-Ping Shen, Jin-Bor Chen, Hui-Li Lin, Chi-Long Hao, Hsueh-Wei Yen, Shyh-Yu Shaw
Pre-germinated brown rice (PGBR) could ameliorate metabolic syndrome, however, not much research estimates the effect of PGBR extract on insulin resistance. The aim of this study is to examine the effects of PGBR extract in TNF-α induced insulin resistance. HepG2 cells, hepatocytes, were cultured in DMEM medium and added with 5 μM insulin or with insulin and 30 ng/ml TNF-α or with insulin, TNF-α and PGBR extract (50, 100, 300 μg/ml). The glucose levels of the medium were decreased by insulin, demonstrating insulin promoted glucose uptake into cell...
January 2018: Kaohsiung Journal of Medical Sciences
https://www.readbyqxmd.com/read/29306837/glycogen-synthase-kinase-3-and-its-inhibitors-potential-target-for-various-therapeutic-conditions
#10
REVIEW
A Prasanth Saraswati, S M Ali Hussaini, Namballa Hari Krishna, Bathini Nagendra Babu, Ahmed Kamal
Glycogen Synthase Kinase-3 (GSK-3) is a serine/threonine kinase which is ubiquitously expressed and is regarded as a regulator for various cellular events and signalling pathways. It exists in two isoforms, GSK-3α and GSK-3β and can phosphorylate a wide range of substrates. Aberrancy in the GSK-3 activity can lead to various diseases like Alzheimer's, diabetes, cancer, neurodegeneration etc., rendering it an attractive target to develop potent and specific inhibitors. The present review focuses on the recent developments in the area of GSK-3 inhibitors and also enlightens its therapeutic applicability in various disease conditions...
December 9, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29299988/an-overview-of-discovery-of-thiazole-containing-heterocycles-as-potent-gsk-3%C3%AE-inhibitors
#11
Deepika Sharma, Anjleena Malhotra, Ranju Bansal
Glycogen synthase kinase-3 (GSK-3) is a multifunctional serine/threonine (ser/thr) kinase that was originally identified as a regulator of glycogen metabolism and coupled with insulin signaling. Due to multifunctionality of this enzyme, it is found to play an important role in the onset and progression of various human diseases. Thiazole nucleus has received special attention by medicinal chemists because of its wide therapeutic potential. The objective of this review is to cover all the aspects of GSK-3β enzyme including its clinical implications, types of inhibitors with special reference to thiazole as GSK-3β inhibitor...
January 4, 2018: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/29277983/thymoquinone-can-improve-neuronal-survival-and-promote-neurogenesis-in-rat-hippocampal-neurons
#12
Merve Beker, Tuğçe Dallı, Birsen Elibol
SCOPE: Thymoquinone (TQ) has been used as a potential therapeutic for diseases such as cancer, and diabetes. Herein, we aimed to investigate the effect of TQ on behavioral and molecular parameters in healthy rat hippocampus. METHODS: TQ (20 mg/kg/day) was administered intragastrically for 15 days to adult rats. After the behavioral tests, the hippocampal tissues were investigated in histological and molecular level. RESULTS: In both DG and CA1, TQ significantly increased the number of hippocampal neurons...
December 26, 2017: Molecular Nutrition & Food Research
https://www.readbyqxmd.com/read/29233065/understanding-the-role-of-glycogen-synthase-kinase-3-in-l-dopa-induced-dyskinesia-in-parkinson-s-disease
#13
Hojin Choi, Seong-Ho Koh
Levodopa (L-DOPA) is the most commonly used drug for Parkinson's disease (PD), but its long-term use is associated with various complications, including L-DOPA-induced dyskinesia (LID). Many studies have suggested that L-DOPA neurotoxicity and LID are associated with glycogen synthase kinase-3 (GSK-3) activation. Areas covered: LID is caused by striatal dopamine (DA) denervation in PD and pulsatile L-DOPA treatment. These factors lead to dysregulated DA transmission, abnormal intracellular signaling and transcription factors in striatal neurons, and altered gene expression and plasticity at corticostriatal synapses...
December 15, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29218434/inhibition-of-gsk-3beta-signaling-pathway-rescues-ketamine-induced-neurotoxicity-in-neural-stem-cell-derived-neurons
#14
Jingjing Zhang, Changlei Cui, Yanhui Li, Haiyang Xu
Clinical application of anesthetic reagent, ketamine (Keta), may induce irreversible neurotoxicity in central nervous system. In this work, we utilized an in vitro model of neural stem cells-derived neurons (nSCNs) to evaluate the role of GSK-3 signaling pathway in Keta-induced neurotoxicity. Embryonic mouse-brain neural stem cells were differentiated into neurons in vitro. Keta (50 μM)-induced neurotoxicity in cultured nSCNs was monitored by apoptosis, immunohistochemical and western blot assays, respectively...
December 7, 2017: Neuromolecular Medicine
https://www.readbyqxmd.com/read/29185832/regulation-of-reactionary-dentine-formation
#15
V C M Neves, P T Sharpe
During the treatment of dental caries that has not penetrated the tooth pulp, maintenance of as much unaffected dentine as possible is a major goal during the physical removal of decayed mineral. Damage to dentine leads to release of fossilized factors (transforming growth factor-β [TGF-β] and bone morphogenic protein [BMP]) in the dentine that are believed to stimulate odontoblasts to secrete new "tertiary" dentine (reactionary dentine). This is formed on the pulpal surface of existing dentine and rethickens the dentine...
November 1, 2017: Journal of Dental Research
https://www.readbyqxmd.com/read/29168273/synergistic-inhibition-of-cell-proliferation-by-combined-targeting-with-kinase-inhibitors-and-dietary-xanthone-is-a-promising-strategy-for-melanoma-treatment
#16
Y Xia, J Sun
α-Mangostin is a dietary xanthone that displays various biological activities, and numerous reports have shown its efficacy in cancer prevention and inhibition. As most agents have been shown to be ineffective as single-agent therapy for malignant melanoma (MM), the principle of targeted chemotherapy for MM is to use effective inhibitors and combination methods. In this study, we tested the cytotoxicity of several kinase inhibitors, including the glycogen synthase kinase (GSK)-3 inhibitor CHIR99021, and rapamycin, in combination with a dietary xanthone, α-mangostin, by screening from a kinase inhibitor library for melanogenesis in SK-MEL-2 MM cells, and verified these by clone formation efficiency, terminal dUTP nick end labelling, and expression of apoptosis-related proteins...
November 22, 2017: Clinical and Experimental Dermatology
https://www.readbyqxmd.com/read/29163854/interactions-between-tgf-%C3%AE-1-canonical-wnt-%C3%AE-catenin-pathway-and-ppar-%C3%AE-in-radiation-induced-fibrosis
#17
REVIEW
Alexandre Vallée, Yves Lecarpentier, Rémy Guillevin, Jean-Noël Vallée
Radiation therapy induces DNA damage and inflammation leading to fibrosis. Fibrosis can occur 4 to 12 months after radiation therapy. This process worsens with time and years. Radiation-induced fibrosis is characterized by fibroblasts proliferation, myofibroblast differentiation, and synthesis of collagen, proteoglycans and extracellular matrix. Myofibroblasts are non-muscle cells that can contract and relax. Myofibroblasts evolve towards irreversible retraction during fibrosis process. In this review, we discussed the interplays between transforming growth factor-β1 (TGF-β1), canonical WNT/β-catenin pathway and peroxisome proliferator-activated receptor gamma (PPAR γ) in regulating the molecular mechanisms underlying the radiation-induced fibrosis, and the potential role of PPAR γ agonists...
October 27, 2017: Oncotarget
https://www.readbyqxmd.com/read/29132216/curcumin-decreases-hyperphosphorylation-of-tau-by-down-regulating-caveolin-1-gsk-3%C3%AE-in-n2a-app695swe-cells-and-app-ps1-double-transgenic-alzheimer-s-disease-mice
#18
Jieyun Sun, Xiong Zhang, Chen Wang, Zhipeng Teng, Yu Li
Caveolin-1, the marker protein of membranal caveolae, is not only involved in cholesterol regulation, but also participates in the cleavage of amyloid [Formula: see text]-protein precursor (APP) and the generation of [Formula: see text]-amyloid peptide. It has been reported to be tightly related with Tau. In our previous studies, curcumin has been confirmed to play a neuroprotective role in Alzheimer's disease (AD), but its effects on Caveolin-1, Tau and their correlation, and the mechanism is still unknown...
2017: American Journal of Chinese Medicine
https://www.readbyqxmd.com/read/29121589/pharmacological-targeting-of-gsk-3-and-nrf2-provides-neuroprotection-in-a-preclinical-model-of-tauopathy
#19
Antonio Cuadrado, Sebastian Kügler, Isabel Lastres-Becker
Tauopathies are a group of neurodegenerative disorders where TAU protein is presented as aggregates or is abnormally phosphorylated, leading to alterations of axonal transport, neuronal death and neuroinflammation. Currently, there is no treatment to slow progression of these diseases. Here, we have investigated whether dimethyl fumarate (DMF), an inducer of the transcription factor NRF2, could mitigate tauopathy in a mouse model. The signaling pathways modulated by DMF were also studied in mouse embryonic fibroblast (MEFs) from wild type or KEAP1-deficient mice...
November 6, 2017: Redox Biology
https://www.readbyqxmd.com/read/29109121/glycogen-synthase-kinase-3-modulates-cbl-b-and-constrains-t-cell-activation
#20
Charles W Tran, Samuel D Saibil, Thierry Le Bihan, Sara R Hamilton, Karl S Lang, Han You, Amy E Lin, Kristine M Garza, Alisha R Elford, Kelly Tai, Michael E Parsons, Kip Wigmore, Mitchell G Vainberg, Josef M Penninger, James R Woodgett, Tak W Mak, Pamela S Ohashi
The decision between T cell activation and tolerance is governed by the spatial and temporal integration of diverse molecular signals and events occurring downstream of TCR and costimulatory or coinhibitory receptor engagement. The PI3K-protein kinase B (PKB; also known as Akt) signaling pathway is a central axis in mediating proximal signaling events of TCR and CD28 engagement in T cells. Perturbation of the PI3K-PKB pathway, or the loss of negative regulators of T cell activation, such as the E3 ubiquitin ligase Cbl-b, have been reported to lead to increased susceptibility to autoimmunity...
November 6, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
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