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Literature summary for 5.6.2.2 extracted from

  • Qi, X.; Hou, S.; Lepp, A.; Li, R.; Basir, Z.; Lou, Z.; Chen, G.
    Phosphorylation and stabilization of topoisomerase IIalpha protein by p38gamma mitogen-activated protein kinase sensitize breast cancer cells to its poisons (2011), J. Biol. Chem., 286, 35883-35890.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 5.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
p38gamma but not p38alpha MAPK is specifically activated by treatment of breast cancer cells with topoisomerase II drug in intrinsically sensitive but not resistant cells, whereas paclitaxel (Taxol) does not have this effect. The activated p38gamma in turn phosphorylates and stabilizes the topoisomerase II protein, and this enhances the growth inhibition by Topo II drugs. p38gamma activity is necessary and sufficient for Topo IIalpha expression, the drug-p38gamma-Topo IIalpha axis is only detected in intrinsically sensitive but not resistant cells Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
co-overexpression of Topo IIalpha with p38gamma protein in primary breast cancer cells using adenoviral-mediated gene delivery, expression of FLAG-tagged enzyme in 293T cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
amsacrine
-
 Homo sapiens
etoposide
-
 Homo sapiens
additional information no inhibition by paclitaxel Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein phosphorylation at Ser1524 and stabilization of topoisomerase IIalpha protein by p38gamma mitogen-activated protein kinase in vivo and in vitro, in vitro kinase assay using recombinant TopoIIalpha and recombinant His-tagged p38gamma Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-
MDA-MB-231 cell
-
 Homo sapiens
-
MDA-MB-468 cell
-
 Homo sapiens
-
T47-D cell
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
topo II
-
 Homo sapiens
Topoisomerase II
-
 Homo sapiens
topoisomerase IIalpha
-
 Homo sapiens

General Information

General Information Comment Organism
physiological function p38gamma but not p38alpha MAPK is specifically activated by treatment of breast cancer cells with topoisomerase II drugs, whereas paclitaxel (Taxol) does not have this effect. The activated p38gamma in turn phosphorylates and stabilizes the topoisomerase II protein, and this enhances the growth inhibition by Topo II drugs. p38gamma activity is necessary and sufficient for Topo IIalpha expression, the drug-p38gamma-Topo IIalpha axis is only detected in intrinsically sensitive but not resistant cells Homo sapiens