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Literature summary for 2.7.11.23 extracted from

  • Nieto Moreno, N.; Villafanez, F.; Giono, L.E.; Cuenca, C.; Soria, G.; Munoz, M.J.; Kornblihtt, A.R.
    GSK-3 is an RNA polymerase II phospho-CTD kinase (2020), Nucleic Acids Res., 48, 6068-6080 .
    View publication on PubMedView publication on EuropePMC

Protein Variants

Protein Variants Comment Organism
K85A kinase-dead mutant of isoform GSK-3beta Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
6-[(2-[[4-(2,4-dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)pyrimidin-2-yl]amino]ethyl)amino]pyridine-3-carbonitrile
-
Homo sapiens
GW779439X 21% inhibition at 0.0001 mM Homo sapiens
GW801372X 33% inhibition at 0.0001 mM Homo sapiens
GW805758X 36% inhibition at 0.0001 mM Homo sapiens
GW806290X 22% inhibition at 0.0001 mM Homo sapiens
GW810578X 26% inhibition at 0.0001 mM Homo sapiens
N-(4-methoxybenzyl)-2-(5-nitro-1,3-thiazol-2-yl)acetamide
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ 10 mM used in assay conditions Homo sapiens
Mn2+ 1 mM used in assay conditions Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
-
Homo sapiens
-
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + [carboxy terminal domain of RNA polymerase II] the enzyme GSK-3 phosphorylates the carboxy terminal domain of RNA polymerase II in vitro, but preferentially when the substrate is previously phosphorylated, consistently with the requirement of a priming phosphorylation reported for GSK-3 efficacy Homo sapiens ADP + phospho-[carboxy terminal domain of RNA polymerase II]
-
?

Synonyms

Synonyms Comment Organism
glycogen synthase kinase 3
-
Homo sapiens
GSK-3
-
Homo sapiens
GSK-3beta isoform Homo sapiens
RNA polymerase II phospho-CTD kinase
-
Homo sapiens
RNAPII phospho-CTD kinase
-
Homo sapiens

General Information

General Information Comment Organism
malfunction enzyme GSK-3 inhibition only prevents CTD hyperphosphorylation triggered by UV but not basal phosphorylation. Enzyme inhibition abrogates both the reduction in RNA polymerase II elongation and changes in AS elicited by UV. GSK-3 inhibition prevents UV-induced apoptosis Homo sapiens
physiological function GSK-3 is a kinase involved in the transcriptional response to UV-induced DNA damage Homo sapiens