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Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors
Bioorganic & Medicinal Chemistry Letters, 2004A series of [1-aryl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]arylhydrazones were discovered as novel inhibitors glycogen synthase kinase-3 (GSK-3). Based on initial modeling a detailed SAR was constructed. Modification of the interior binding aryl ring (Ar(1)) determined this to be a tight binding region with little room for modification. As predicted from the
Frank Preugschat+12 more
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GSK-3 parameters in lymphocytes of schizophrenic patients
Psychiatry Research, 2002Glycogen synthase kinase-3 (GSK-3) is a highly conserved serine/threonine protein kinase that is involved in the signal transduction cascades of multiple cellular processes. GSK-3 has two isoforms, designated alpha and beta. GSK-3beta protein levels and GSK-3 enzyme activity have been reported to be reduced by over 40% in postmortem frontal cortex of ...
Carmit Nadri+3 more
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GSK‐3: A key player in neurodegeneration and memory
IUBMB Life, 2009AbstractAbnormalities in molecular signalling have been implicated in neurodegeneration. It is emerging that glycogen synthase kinase‐3 (GSK‐3) is a key signalling molecule that induces neurodegeneration and deficits in memory formation related to Alzheimer's disease (AD).
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GSK-3 is essential in the pathogenesis of Alzheimer's disease
Journal of Alzheimer's Disease, 2006Glycogen synthase kinase-3 (GSK-3) is a pivotal molecule in the development of Alzheimer's disease (AD). GSK-3beta is involved in the formation of paired helical filament (PHF)-tau, which is an integral component of the neurofibrillary tangle (NFT) deposits that disrupt neuronal function, and a marker of neurodegeneration in AD.
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Novel GSK‐3 Inhibitor with Improved Cellular Activity.
ChemInform, 2004AbstractFor Abstract see ChemInform Abstract in Full Text.
Stephen A. Thomson+7 more
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GSK-3 as a novel prognostic indicator in leukemia
Advances in Biological Regulation, 2017While leukemias represent a diverse set of diseases with malignant cells derived from myeloid or lymphoid origin, a common feature is the dysregulation of signal transduction pathways that influence leukemogeneisis, promote drug resistance, and favor leukemia stem cells.
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Cancer Biotherapy and Radiopharmaceuticals
Background: Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase known to participate in the regulation of β-catenin signaling (Wnt signaling). This aids in the establishment of a multicomponent destruction complex that stimulates phosphorylation, leading to the destruction of β-catenin.
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Background: Glycogen synthase kinase-3 (GSK-3) is a serine/threonine kinase known to participate in the regulation of β-catenin signaling (Wnt signaling). This aids in the establishment of a multicomponent destruction complex that stimulates phosphorylation, leading to the destruction of β-catenin.
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Science Signaling, 2008
Cross-talk between signaling pathways alters transcriptional regulatory activity of the glucocorticoid nuclear receptor.
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Cross-talk between signaling pathways alters transcriptional regulatory activity of the glucocorticoid nuclear receptor.
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