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Literature summary for 2.7.11.26 extracted from

  • Santo, L.; Vallet, S.; Hideshima, T.; Cirstea, D.; Ikeda, H.; Pozzi, S.; Patel, K.; Okawa, Y.; Gorgun, G.; Perrone, G.; Calabrese, E.; Yule, M.; Squires, M.; Ladetto, M.; Boccadoro, M.; Richardson, P.G.; Munshi, N.C.; Anderson, K.C.; Raje, N.
    AT7519, a novel small molecule multi-cyclin-dependent kinase inhibitor, induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition (2010), Oncogene, 29, 2325-2336.
    View publication on PubMedView publication on EuropePMC
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Activating Compound

Activating Compound Comment Organism Structure
AT7519 0.0005 mM AT7519 inhibits glycogen synthase kinase 3beta phosphorylation, AT7519 dephosphorylates GSK-3beta independent of inhibition of transcription Homo sapiens

Application

Application Comment Organism
medicine GSK-3beta is a therapeutic target in cancer treatment Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + beta-catenin Homo sapiens
-
 ADP + phosphorylated beta-catenin
-
 ?
ATP + c-Myc Homo sapiens
-
 ADP + phosphorylated c-Myc
-
 ?
ATP + cyclin D Homo sapiens
-
 ADP + phosphorylated cyclin D
-
 ?
ATP + cyclin E Homo sapiens
-
 ADP + phosphorylated cyclin E
-
 ?
ATP + glycogen synthase Homo sapiens
-
 ADP + glycogen synthase phosphate
-
 ?
ATP + nuclear factor-kappaB Homo sapiens
-
 ADP + phosphorylated nuclear factor-kappaB
-
 ?
ATP + p53 Homo sapiens
-
 ADP + phosphorylated p53
-
 ?
ATP + protein tau Homo sapiens
-
 ADP + protein tau phosphate
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein GSK-3beta is activated via phosphorylation at Ser9 Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
MM1-S cell
-
 Homo sapiens
-
multiple myeloma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + beta-catenin
-
 Homo sapiens ADP + phosphorylated beta-catenin
-
 ?
ATP + c-Myc
-
 Homo sapiens ADP + phosphorylated c-Myc
-
 ?
ATP + cyclin D
-
 Homo sapiens ADP + phosphorylated cyclin D
-
 ?
ATP + cyclin E
-
 Homo sapiens ADP + phosphorylated cyclin E
-
 ?
ATP + glycogen synthase
-
 Homo sapiens ADP + glycogen synthase phosphate
-
 ?
ATP + nuclear factor-kappaB
-
 Homo sapiens ADP + phosphorylated nuclear factor-kappaB
-
 ?
ATP + p53
-
 Homo sapiens ADP + phosphorylated p53
-
 ?
ATP + protein tau
-
 Homo sapiens ADP + protein tau phosphate
-
 ?

Synonyms

Synonyms Comment Organism
glycogen synthase kinase-3beta
-
 Homo sapiens
GSK-3beta
-
 Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
 Homo sapiens