Trypanosoma brucei Glycogen Synthase Kinase-3, A Target for
Ojo KK, Gillespie JR, Riechers AJ, Napuli AJ, Verlinde CL, et al. Glycogen synthase kinase 3 is a potential drug target for African trypanosomiasis therapy. Antimicrob Agents Chemother. ; 52:3710–3717. [PMC free article]
Glycogen Synthase Kinase 3 Inhibitors in the Next Horizon
06/30 · Glycogen synthase kinase 3 (GSK-3), a proline/serine protein kinase ubiquitously expressed and involved in many cellular signaling pathways, plays a key role in the pathogenesis of Alzheimer's disease (AD) being probably the link between β-amyloid and tau pathology. A great effort has recently been done in the discovery and development of different new molecules, of synthetic and
Frontiers | Glycogen Synthase Kinase-3: A Promising
Glycogen synthase kinase-3 is a serine/threonine kinase that exists in two isoforms, GSK3α and GSK3β (Woodgett, 1990). Regulation of GSK3 is primarily mediated by inhibitory serine-phosphorylation, specifically at ser21 of
Glycogen synthase kinase‐3 is required for optimal de novo
Studies have shown that the inositol biosynthetic pathway and the enzyme glycogen synthase kinase‐3 (GSK‐3) are targets of the mood‐stabilizing drugs lithium and valproate. However, a relationship between these targets has not been previously described.
Glycogen synthase kinase 3: a drug target for CNS therapies
From a drug discovery standpoint, any potential side inhibited by glycogen synthase kinase-3 beta and facilitated by lithium.J.Neurochem.78,1219–1232.
Glycogen Synthase Kinase 3 in Cancer Biology and Treatment
Glycogen synthase kinase (GSK)3 is an isoform of the GSK3 family of kinases. It regulates It regulates many fundamental biological processes in cells by phosphorylating serine and threonine residues
Glycogen synthase kinase-3: a potential preventive target for
Glycogen synthase kinase-3 (GSK-3, α and β) is a protein serine/threonine kinase and has diverse cellular functions and numerous substrates. We sought to summarize all the studies done with GSK-3 in prostate cancers and to provide a prospective direction for future work.
Glycogen Synthase Kinase-3 (GSK-3)-Targeted Therapy and
02/17 · Potential role of glycogen synthase kinase-3 in skeletal muscle insulin resistance of type 2 diabetes. Diabetes. 2000;49:263-71 7. Watkins CC, Sawa A, Pomper MG. Glia and immune cell signaling in bipolar disorder: insights. 4
Subtly Modulating Glycogen Synthase Kinase 3 β: Allosteric
Subtly Modulating Glycogen Synthase Kinase 3 β: Allosteric Inhibitor Development and Their Potential for the Treatment of Chronic Diseases Glycogen synthase kinase 3 β (GSK-3β) is a central target in several unmet diseases.
Screening of inhibitors of Taenia solium glycogen synthase
Glycogen synthase kinase-3 (GSK-3) is a widely conserved family of protein kinases that was identi ed to regulate glycogen metabolism in the 1970s. 15 In higher
Glycogen synthase kinase-3 inhibitor as a multi-targeting anti
07/01 · Glycogen synthase kinase-3 (GSK-3) GSK-3 is a serine/threonine kinase that was originally identified as a key regulatory enzyme in glycogen metabolism  . However, this serine/threonine kinase is now known to regulate numerous cellular processes through a number of signaling pathways important for cell proliferation, stem cell renewal, apoptosis, and development  .
Pharmacological inhibition of glycogen synthase kinase 3
02/01 · Bijur GN, Jope RS (2003) Glycogen synthase kinase-3 beta is highly activated in nuclei and mitochondria. Neuroreport 14:2415–2419.  [Google Scholar] Cai Z, Zhao Y, Zhao B ( ) Roles of glycogen synthase kinase 3 in. 9] 
Glycogen synthase kinase 3: a drug target for CNS therapies
Abstract Glycogen synthase kinase3 (GSK3) is emerging as a prominent drug target in the CNS. The most exciting of the possibilities of GSK3 lies within the treatment of Alzheimer's disease (AD) where abnormal increases in GSK3 levels and activity have been associated with neuronal death, paired helical filament tau formation and neurite retraction as well as a decline in cognitive performance.
First Non-ATP Competitive Glycogen Synthase Kinase 3
Glycogen synthase kinase 3 β (GSK-3β) has a central role in Alzheimer's disease (AD). Selective inhibitors which avoid τ hyperphosphorylation may represent an effective therapeutical approach to the AD pharmacotherapy and other neurodegenerative disorders. Here, we describe the synthesis, biological evaluation, and SAR of the small heterocyclic thiadiazolidinones (TDZD) as the first non-ATP
Glycogen Synthase Kinase 3 (GSK3) inhibitor Pipeline Insight
The "Glycogen Synthase Kinase 3 (GSK3) inhibitor - Pipeline Insight, " drug pipelines has been added to ResearchAndMarkets.com's offering.
Multiple Roles for Glycogen Synthase Kinase-3 as a Drug
Recent evidence implicates the protein kinase glycogen synthase kinase 3 (GSK-3) in the regulation of both of these processes. GSK-3 has long been studied as one of several tau protein kinases, and has more recently been shown to be involved in the generation of Aβ peptides.
GSK3 inhibitors: development and therapeutic potential
2004/06/01 · In the late 1970s, glycogen synthase kinase-3 (GSK3) was identified as a protein kinase that inactivates glycogen synthase, but was ignored as a drug
Effects of a Novel Glycogen Synthase Kinase-3 Inhibitor on
2002/10/01 · Therefore, activation of glycogen synthase through inhibition of glycogen synthase kinase (GSK)-3 represents a potential new therapeutic target. To examine this possibility, we performed oral glucose tolerance tests (OGTTs) and euglycemic-insulinemic clamp studies in Zucker diabetic fatty ( fa / fa ) rats before and after treatment with novel GSK-3 inhibitors.
PDF) Glycogen Synthase Kinase 3 as an Anticancer Drug Target
Glycogen Synthase Kinase-3 (GSK-3) is a constitutively acting multifunctional serine/threonine kinase, a role of which has been marked in several physiological pathways, making it a potential
A tale of (glycogen synthase kinase) three: Lithium, the
Nevertheless, there is some interest in the potential role of these drugs in inflammatory pathways regulation including those path-ways in the setting of acute kidney injury (AKI). This therapeutic potential is based on lithium-induced inhibitory phos - phorylation of glycogen synthase kinase-3 beta (GSK3b), a protein related
Glycogen Synthase Kinase-3: a Putative Molecular Target
Among these is glycogen synthase kinase-3 (GSK-3). Recent preclinical evidence, including biochemical, pharmacological, genetic, and rodent behavioral models, supports the hypothesis that
AR-A014418 as a glycogen synthase kinase-3 inhibitor: anti
AR-A014418 as a glycogen synthase kinase-3 inhibitor: anti-apoptotic and therapeutic potential in experimental spinal cord injury. Tunçdemir M (1), Yıldırım A, Karaoğlan A, Akdemir O, Oztürk M.
Glycogen Synthase Kinase 3 (GSK3) inhibitor - Pipeline
02/01 · Glycogen-synthase kinase-3 (GSK3) exists in two isoforms, termed α and β, which are generated from distinct genes. GSK3 is active in its basal state and is inhibited upon phosphorylation at Ser9 in GSK-3β and at Ser21 in
Glycogen synthase kinase 3:an - Cell
Glycogen synthase kinase 3 (GSK-3) is a serine/threonine protein kinase that has recently emerged as a key target in drug discovery.It has been implicated in multiple cellular processes and linked with the pathogenesis of several diseases.
Evaluation of Glycogen Synthase Kinase 3 as a drug target in
This thesis aims at evaluating the essentiality of Glycogen Synthase Kinase 3 (TbGSK3 short; Tb927.10.13780) and chemically validating it as a potential drug target in T. brucei. TbGSK3 recombinant protein was biochemically
Glycogen synthase kinase-3 inhibition as a potential
May 01, · We have systematically collected and analyzed the biomedical literature and then validated the most promising drug target, i.e., GSK-3. Pharmacological inhibition of glycogen synthase kinase-3 enzyme successfully attenuated the cognitive disabilities under mild chronic cerebral hypoperfusion which mimic core features of vascular dementia.
In silico docking and comparative ADMET profile of different
Glycogen synthase kinase 3 beta (GSK3 β) plays a key role in pathologic hyper phosphorylation of tau and plays an important role in the pathogenesis of Alzheimer's disease. In the present study, we have screened a set of potential hits in in silico platform to gain insight regarding binding profile with the target (GSK3 β) from molecular
Exploiting an Asp-Glu “switch” in glycogen synthase kinase 3
The enzyme glycogen synthase kinase 3 (GSK3) has been proposed as a potential therapeutic target in many diseases, but none of the drugs targeting this enzyme so far have translated to the clinic. A major reason for this failure to translate is the existence of two closely related paralogs of GSK3 such that most drugs target both forms at once and cause unacceptable toxicity. By applying a
Hindawi Publishing Corporation - Glycogen Synthase Kinase 3
11/28 · Glycogen synthase kinase 3β (GSK-3β) is a widely expressed kinase with distinct functions in different types of cells. The role of GSK-3 β in regulating innate immune activation has been well documented, but as far as we know, its role in POCD has not been fully elucidated.
Glycogen Synthase Kinase 3 Is a Potential Drug Target for
In this study, we evaluated the validity of Trypanosoma brucei glycogen synthase kinase 3 (GSK-3) as a potential drug target. Interference with the RNA of either of two GSK-3 homologues in bloodstream-form T. brucei parasites led to growth arrest and altered parasite morphology, demonstrating their requirement for cell survival.
Glycogen Synthase Kinase-3β Is a Functional Modulator of
06/01 · Glycogen synthase kinase-3 (GSK3) is a constitutively active protein kinase that is involved in neuronal regulation and is a potential pharmacological target of neurological disorders. We found previously that GSK3β selectively interacts with 5-hydroxytryptamine-1B receptors (5-HT1BR) that have important functions in serotonin neurotransmission and behavior. In this study, we provide new