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Literature summary for 2.7.11.1 extracted from

  • Kotliarova, S.; Pastorino, S.; Kovell, L.C.; Kotliarov, Y.; Song, H.; Zhang, W.; Bailey, R.; Maric, D.; Zenklusen, J.C.; Lee, J.; Fine, H.A.
    Glycogen synthase kinase-3 inhibition induces glioma cell death through c-MYC, nuclear factor-kappaB, and glucose regulation (2008), Cancer Res., 68, 6643-6651.
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine GSK3 is an important therapeutic target for gliomas Homo sapiens

Protein Variants

Protein Variants Comment Organism
additional information down-regulation of GSK3 activity results in alteration of intracellular glucose metabolism resulting in dissociation of hexokinase II from the outer mitochondrial membrane with subsequent mitochondrial destabilization Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
enzastaurin activation-related phosphorylation of Y216/Y276 is dramatically decreased following exposure to enzastaurin whereas the inhibitory phosphorylation of S21 is significantly up-regulated in glioma cells. GSK3 inhibition results in glioma cell death and reduced tumorigenicity Homo sapiens
additional information inhibition of GSK3 activity results in c-MYC activation, leading to the induction of Bax, Bim, DR4/DR5, and tumor necrosis factor-related apoptosis-inducing ligand expression and subsequent cytotoxicity. inhibition of GSK3 activity causes a dramatic decrease in intracellular nuclear factor-kappaB activity. Inhibition of GSK3 activity results in c-MYC-dependent glioma cell death through multiple mechanisms, all of which converge on the apoptotic pathways Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein
-
Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
glioma cell line U251, T98, U87, U373, U118, A172 Homo sapiens
-

Synonyms

Synonyms Comment Organism
glycogen synthase kinase 3
-
Homo sapiens
GSK3
-
Homo sapiens
serine-threonine kinase
-
Homo sapiens