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 (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 | Comment | Organism | Structure |
---|---|---|---|
amsacrine | - |
Homo sapiens | |
etoposide | - |
Homo sapiens | |
additional information | no inhibition by paclitaxel | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
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 | 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 | Comment | Organism |
---|---|---|
topo II | - |
Homo sapiens |
Topoisomerase II | - |
Homo sapiens |
topoisomerase IIalpha | - |
Homo sapiens |
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 |