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https://www.readbyqxmd.com/read/28186681/skin-derived-precursors-as-a-source-of-progenitors-for-corneal-endothelial-regeneration
#1
Emi Inagaki, Shin Hatou, Kazunari Higa, Satoru Yoshida, Shinsuke Shibata, Hideyuki Okano, Kazuo Tsubota, Shigeto Shimmura
Corneal blindness is the fourth leading cause of blindness in the world. Current treatment is allogenic corneal transplantation, which is limited by shortage of donors and immunological rejection. Skin-derived precursors (SKPs) are postnatal stem cells, which are self-renewing, multipotent precursors that can be isolated and expanded from the dermis. Facial skin may therefore be an accessible autologous source of neural crest derived cells. SKPs were isolated from facial skin of Wnt1-Cre/Floxed EGFP mouse. After inducing differentiation with medium containing retinoic acid and GSK 3-β inhibitor, SKPs formed polygonal corneal endothelial-like cells (sTECE)...
February 6, 2017: Stem Cells Translational Medicine
https://www.readbyqxmd.com/read/28140405/the-impact-of-disrupted-in-schizophrenia-1-disc1-on-the-dopaminergic-system-a-systematic-review
#2
REVIEW
T Dahoun, S V Trossbach, N J Brandon, C Korth, O D Howes
Disrupted-in-Schizophrenia 1 (DISC1) is a gene known as a risk factor for mental illnesses possibly associated with dopamine impairments. DISC1 is a scaffold protein interacting with proteins involved in the dopamine system. Here we summarise the impact of DISC1 disruption on the dopamine system in animal models, considering its effects on presynaptic dopaminergic function (tyrosine hydroxylase levels, dopamine transporter levels, dopamine levels at baseline and after amphetamine administration) and postsynaptic dopaminergic function (dopamine D1 and D2 receptor levels, dopamine receptor-binding potential and locomotor activity after amphetamine administration)...
January 31, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28130417/phosphorylation-of-clustered-serine-residues-in-the-n-terminus-of-bps-domain-negatively-regulates-formation-of-the-complex-between-human-grb14-and-insulin-receptor
#3
Junichi Taira, Yutaka Kida, Kohei Inatomi, Hideyuki Komatsu, Yuichiro Higashimoto, Hiroshi Sakamoto
Growth factor receptor-bound protein 14 (Grb14) is a negative regulator of insulin receptor (IR) and is involved in a negative feedback mechanism of insulin signaling. Grb14 associates with IR and inhibits its tyrosine kinase activity through the between pleckstrin homology and Src homology-2 (BPS) domain. We previously reported that the pharmacological inhibition and knockdown of glycogen synthase kinase-3 (GSK-3) facilitates the insulin-induced complex formation of human Grb14 (hGrb14) and IR, suggesting that GSK-3 suppresses hGrb14 recruitment to IR...
January 27, 2017: Journal of Biochemistry
https://www.readbyqxmd.com/read/28129131/6bio-enhances-oligonucleotide-activity-in-cells-a-potential-combinatorial-anti-androgen-receptor-therapy-in-prostate-cancer-cells
#4
Xiaowei Zhang, Daniela Castanotto, Sangkil Nam, David Horne, Cy Stein
Approximately 15%-25% of men diagnosed with prostate cancer do not survive their disease. The American Cancer Society estimated that for the year 2016 the number of prostate cancer deaths will be 26,120. Thus, there is a critical need for novel approaches to treat this deadly disease. Using high-throughput small-molecule screening, we found that the small molecule 6-bromo-indirubin-3'-oxime (6BIO) significantly improves the targeting of antisense oligonucleotides (ASOs) delivered by gymnosis (i.e., in the absence of any transfection reagents) in both the cell cytoplasm and the nucleus...
January 4, 2017: Molecular Therapy: the Journal of the American Society of Gene Therapy
https://www.readbyqxmd.com/read/28119025/synthesis-of-carbon-11-labeled-isonicotinamides-as-new-potential-pet-agents-for-imaging-of-gsk-3-enzyme-in-alzheimer-s-disease
#5
Mingzhang Gao, Min Wang, Qi-Huang Zheng
The authentic standards 2-(cyclopropanecarboxamido)-N-(4-methoxypyridin-3-yl)isonicotinamide (4a) and 2-(cyclopropanecarboxamido)-N-(4-(4-methoxyphenyl)pyridin-3-yl)isonicotinamide (7a), and their corresponding precursors 2-(cyclopropanecarboxamido)-N-(4-hydroxypyridin-3-yl)isonicotinamide (4b) and 2-(cyclopropanecarboxamido)-N-(4-(4-hydroxyphenyl)pyridin-3-yl)isonicotinamide (7b) were synthesized from methyl 2-aminoisonicotinate and cyclopropanecarbonyl chloride with overall chemical yield 47% in three steps, 22% in four steps, 40% in three steps, and 17% in four steps, respectively...
January 16, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28114834/small-molecules-targeting-glycogen-synthase-kinase-3-as-potential-drug-candidates-for-the-treatment-of-retinitis-pigmentosa
#6
Miguel Marchena, Beatriz Villarejo-Zori, Josefa Zaldivar-Diez, Valle Palomo, Carmen Gil, Catalina Hernández-Sánchez, Ana Martínez, Enrique J de la Rosa
Retinitis pigmentosa (RP) is an inherited retinal dystrophy that courses with progressive degeneration of retinal tissue and loss of vision. Currently, RP is an unpreventable, incurable condition. We propose glycogen synthase kinase 3 (GSK-3) inhibitors as potential leads for retinal cell neuroprotection, since the retina is also a part of the central nervous system and GSK-3 inhibitors are potent neuroprotectant agents. Using a chemical genetic approach, diverse small molecules with different potency and binding mode to GSK-3 have been used to validate and confirm GSK-3 as a pharmacological target for RP...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28108896/pharmacophore-based-screening-and-drug-repurposing-exemplified-on-glycogen-synthase-kinase-3-inhibitors
#7
Luminita Crisan, Sorin Avram, Liliana Pacureanu
The current study was conducted to elaborate a novel pharmacophore model to accurately map selective glycogen synthase kinase-3 (GSK-3) inhibitors, and perform virtual screening and drug repurposing. Pharmacophore modeling was developed using PHASE on a data set of 203 maleimides. Two benchmarking validation data sets with focus on selectivity were assembled using ChEMBL and PubChem GSK-3 confirmatory assays. A drug repurposing experiment linking pharmacophore matching with drug information originating from multiple data sources was performed...
January 21, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28106616/lymphocyte-phospho-ser-9-gsk-3%C3%AE-total-gsk-3%C3%AE-protein-levels-ratio-is-not-affected-by-chronic-lithium-or-valproate-treatment-in-euthymic-patients-with-bipolar-disorder
#8
Abed N Azab, Ella Vainer, Galila Agam, Yuly Bersudsky
BACKGROUND: Glycogen synthase kinase-3 (GSK-3) inhibition by lithium has been well established in vitro, but proof that this biochemical effect mediates lithium's beneficial action in patients with bipolar disorder is lacking. We studied whether lymphocyte GSK-3β activity measured indirectly in lithium- or valproate (VPA)-treated euthymic patients with bipolar disorder is different from controls. METHODS: Lymphocyte total and Ser-9-phospho-GSK-3β (inactive) levels were measured by Western blotting...
January 19, 2017: Journal of Clinical Psychopharmacology
https://www.readbyqxmd.com/read/28098905/cripto-1-promotes-epithelial-mesenchymal-transition-in-prostate-cancer-via-wnt-%C3%AE-catenin-signaling
#9
Yan Liu, Zhenbang Qin, Kuo Yang, Ranlu Liu, Yong Xu
The Cripto-1 (CR-1) derived EGF-CFC family was overexpressed in tumor development enhancing proliferation, epithelial-mesenchymal transition (EMT) and migration of tumor cells. However, correlation between CR-1 and prostate cancer (PCa) remains still unclear. In the present study, we proved that CR-1 was expressed in PCa and its function was in the progression of PCa. Compared with benign prostatic hyperplasia (BPH) tissues, we confirmed that PCa tissues had high expression of CR-1 by immunohistochemistry and statistical data showed that CR-1 promoted properties of EMT in PCa tissues, including the downregulation of the cell adhesion molecules β-catenin (membrane) and E-cadherin while upregulating transcription factors β-catenin...
January 17, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28093982/pde7-selective-and-dual-inhibitors-advances-in-chemical-and-biological-research
#10
Agnieszka Jankowska, Artur Świerczek, Grażyna Chłoń-Rzepa, Maciej Pawłowski, Elżbieta Wyska
Phosphodiesterase 7 (PDE7) is an intracellular enzyme that specifically hydrolyses the second messenger, cyclic-3',5'-adenosine monophosphate (cAMP), into inactive non-cyclic nucleotide, 5'-AMP. To date, many structurally diverse compounds with PDE7 inhibitory properties have been described, including selective PDE7 inhibitors, dual PDE4/PDE7, PDE7/PDE8, and PDE7/GSK-3 inhibitors, and non-selective PDE inhibitors with high affinity for PDE7. Inhibitors of PDE7 provided beneficial effects in animal models of inflammatory and neurological disorders, including Alzheimer's disease, Parkinson's disease, multiple sclerosis, and many others...
16, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28093238/a-model-of-the-mitochondrial-basis-of-bipolar-disorder
#11
REVIEW
Gerwyn Morris, Ken Walder, Sean L McGee, Olivia M Dean, Susannah J Tye, Michael Maes, Michael Berk
BACKGROUND: Bipolar disorder phenomenologically is a biphasic disorder of energy availability; increased in mania and decreased in depression. In consort, there is accumulating evidence indicating increased mitochondrial respiration and ATP production in bipolar mania which contrasts with decreased mitochondrial function in patients in the euthymic or depressive phase of the illness. Consequently, the central thesis of this paper is that bipolar disorder is due to a phasic dysregulation of mitochondrial biogenergetics...
January 14, 2017: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/28067250/promotion-of-natural-tooth-repair-by-small-molecule-gsk3-antagonists
#12
Vitor C M Neves, Rebecca Babb, Dhivya Chandrasekaran, Paul T Sharpe
The restoration of dentine lost in deep caries lesions in teeth is a routine and common treatment that involves the use of inorganic cements based on calcium or silicon-based mineral aggregates. Such cements remain in the tooth and fail to degrade and thus normal mineral volume is never completely restored. Here we describe a novel, biological approach to dentine restoration that stimulates the natural formation of reparative dentine via the mobilisation of resident stem cells in the tooth pulp. Biodegradable, clinically-approved collagen sponges are used to deliver low doses of small molecule glycogen synthase kinase (GSK-3) antagonists that promote the natural processes of reparative dentine formation to completely restore dentine...
January 9, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28060847/enhanced-chondrogenic-differentiation-of-human-umbilical-cord-wharton-s-jelly-derived-mesenchymal-stem-cells-by-gsk-3-inhibitors
#13
Prapot Tanthaisong, Sumeth Imsoonthornruksa, Apichart Ngernsoungnern, Piyada Ngernsoungnern, Mariena Ketudat-Cairns, Rangsun Parnpai
Articular cartilage is an avascular, alymphatic, and aneural system with very low regeneration potential because of its limited capacity for self-repair. Mesenchymal stem cells (MSCs) are the preferred choice for cell-based therapies. Glycogen synthase kinase 3 (GSK-3) inhibitors are compounds that can induce the Wnt signaling pathway, which is involved in chondrogenesis and cartilage development. Here, we investigated the influence of lithium chloride (LiCl) and SB216763 synergistically with TGF-β3 on chondrogenic differentiation in human mesenchymal stem cells derived from Wharton's jelly tissue (hWJ-MSCs)...
2017: PloS One
https://www.readbyqxmd.com/read/28053024/molecular-pathways-revisiting-glycogen-synthase-kinase-3%C3%AE-as-a-target-for-the-treatment-of-cancer
#14
Amy Walz, Andrey Ugolkov, Sunandana Chandra, Alan Kozikowski, Benedito A Carneiro, Thomas V O'Halloran, Francis J Giles, Daniel D Billadeau, Andrew P Mazar
Glycogen synthase kinase-3β (GSK-3β), a serine/threonine protein kinase, is a complex regulator of numerous cellular functions. GSK-3β is a unique kinase which is constitutively active in resting and non-stimulated cells. GSK-3β has been implicated in a wide range of diseases including neurodegeneration, inflammation and fibrosis, noninsulin-dependent diabetes mellitus, and cancer. It is a regulator of NF-κB-mediated survival of cancer cells, which provided a rationale for the development of GSK-3 inhibitors targeting malignant tumors...
January 4, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28012947/the-gsk-3-inhibitor-vp2-51-produces-antidepressant-effects-associated-with-adult-hippocampal-neurogenesis
#15
Paloma Pérez-Domper, Valle Palomo, Simona Gradari, Carmen Gil, María L de Ceballos, Ana Martínez, Jose Luis Trejo
Glycogen synthase kinase 3 (GSK-3) is a constitutively active kinase that has been implicated in the mechanism of action of mood stabilizers. According to the neurogenic hypothesis of depression, newborn neurons in the adult dentate gyrus are required for the antidepressant effects of certain agents. We demonstrate that administration of the GSK-3 inhibitor VP2.51 (2.5 mg/kg ip, for 3.5 weeks) increases cell proliferation (pH3(+) cells), as well as the short- and long-term survival of newborn neurons (assessed by the 24 h survival of BrdU(+) and DCX(+) neurons), while significantly increasing the commitment of cells to the granule neuron lineage (Prox1 immunoreactivity)...
December 22, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27999207/roles-of-gsk-3-and-micrornas-on-epithelial-mesenchymal-transition-and-cancer-stem-cells
#16
REVIEW
James A McCubrey, Timothy L Fitzgerald, Li V Yang, Kvin Lertpiriyapong, Linda S Steelman, Stephen L Abrams, Giuseppe Montalto, Melchiorre Cervello, Luca M Neri, Lucio Cocco, Alberto M Martelli, Piotr Laidler, Joanna DuliÅ Ska-Litewka, Dariusz Rakus, Agnieszka Gizak, Ferdinando Nicoletti, Luca Falzone, Saverio Candido, Massimo Libra
Various signaling pathways exert critical roles in the epithelial to mesenchymal transition (EMT) and cancer stem cells (CSCs). The Wnt/beta-catenin, PI3K/PTEN/Akt/mTORC, Ras/Raf/MEK/ERK, hedgehog (Hh), Notch and TP53 pathways elicit essential regulatory influences on cancer initiation, EMT and progression. A common kinase involved in all these pathways is moon-lighting kinase glycogen synthase kinase-3 (GSK-3). These pathways are also regulated by micro-RNAs (miRs). TP53 and components of these pathways can regulate the expression of miRs...
December 16, 2016: Oncotarget
https://www.readbyqxmd.com/read/27902447/a-unique-type-of-gsk-3-inhibitor-brings-new-opportunities-to-the-clinic
#17
Avital Licht-Murava, Rom Paz, Lilach Vaks, Limor Avrahami, Batya Plotkin, Miriam Eisenstein, Hagit Eldar-Finkelman
Development of protein kinase inhibitors is a focus of many drug discovery programs. A major problem, however, is the limited specificity of the commonly used adenosine triphosphate-competitive inhibitors and the weak inhibition of the more selective substrate-competitive inhibitors. Glycogen synthase kinase-3 (GSK-3) is a promising drug target for treating neurodegenerative disorders, including Alzheimer's disease (AD), but most GSK-3 inhibitors have not reached the clinic. We describe a new type of GSK-3 inhibitor, L807mts, that acts through a substrate-to-inhibitor conversion mechanism that occurs within the catalytic site of the enzyme...
November 15, 2016: Science Signaling
https://www.readbyqxmd.com/read/27902446/science-signaling-podcast-for-15-november-2016-a-new-type-of-kinase-inhibitor
#18
Hagit Eldar-Finkelman, Annalisa M VanHook
This Podcast features an interview with Hagit Eldar-Finkelman, author of a Research Article that appears in the 15 November 2016 issue of Science Signaling, about a newly developed inhibitor of glycogen synthase kinase 3 (GSK-3). GSK-3 participates in several signaling networks and has been implicated in various pathologies, including neurodegenerative diseases, cognitive impairments, and cancer. Licht-Murava et al developed L807mts, a substrate-competitive peptide inhibitor that blocks GSK-3 activity through an unusual mechanism...
November 15, 2016: Science Signaling
https://www.readbyqxmd.com/read/27901086/glycycoumarin-inhibits-hepatocyte-lipoapoptosis-through-activation-of-autophagy-and-inhibition-of-er-stress-gsk-3-mediated-mitochondrial-pathway
#19
Enxiang Zhang, Shutao Yin, Xinhua Song, Lihong Fan, Hongbo Hu
Herbal medicine as an alternative approach in the treatment of disease has drawn growing attention. Identification of the active ingredient is needed for effective utilization of the herbal medicine. Licorice is a popular herbal plant that is widely used to treat various diseases including liver diseases. Glycycoumarin (GCM) is a representative of courmarin compounds isolated from licorice. In the present study, the protective effect of GCM on hepatocyte lipoapoptosis has been evaluated using both cell culture model of palmitate-induced lipoapoptosis and animal model of non-alcoholic steatohepatitis (NASH)...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27900801/gsk-3-a-key-regulatory-target-for-ketamine-s-rapid-antidepressant-effects-mediated-by-enhanced-ampa-to-nmda%C3%A2-throughput
#20
Carlos A Zarate, Rodrigo Machado-Vieira
No abstract text is available yet for this article.
December 2016: Bipolar Disorders
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