Relation Results

Summary

Name TOP2A
Full Name DNA topoisomerase 2-alpha
Synonyms DNA topoisomerase II, alpha isozyme | TOP2
Primary ID P11388
Links - -
Type protein
Relations 30
Inhibitors idarubicin; Doxorubicin hydrochloride; doxorubicin; Daunorubicin hydrochloride; 4'-epidoxorubicin; etoposide; valrubicin; teniposide; 2-(Decan-2-ylamino)ethyl 4-aminobenzoate
Function Key decatenating enzyme that alters DNA topology by binding to two double-stranded DNA molecules, generating a double-stranded break in one of the str ...
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Type: Score: Layout: SPV 
0.5370.4910.3540.6090.3630.3630.2710.3480.20.80.2740.80.80.80.80.80.70.80.70.20.80.8CDK1TOP2APLK1GSK3BCSNK2A1PRKCBPRKCGPLK3SCF-FBW7YAP/TAZidarubicinNFYDoxorubicin hydrochloridedoxorubicinDaunorubicin hydrochloride4'-epidoxorubicinetoposideSurvivalvalrubicinChromosome_segregationYAP1teniposide2-(Decan-2-ylamino)ethyl 4-aminobenzoate

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▶Modifications Tables

Relations
Regulator
Mechanism
target
score ℹ
+ CDK1 img/unknown.png phosphorylation TOP2A 0.537
Identifier Residue Sequence Organism Cell Line
SIGNOR-30244 Ser1247 KNENTEGsPQEDGVE Homo sapiens HeLa Cell
pmid sentence
We show that many of the sites phosphorylated on topoisomerase iia in vivo correspond to sites phosphorylated in vitro by both p3pdcz and mitogen-activated protein (map) kinase. similarly, phosphopeptide 4 was absent from a mutant protein lacking ser1246
Identifier Residue Sequence Organism Cell Line
SIGNOR-30248 Ser1354 DFVPSDAsPPKTKTS Homo sapiens HeLa Cell
pmid sentence
We show that many of the sites phosphorylated on topoisomerase iia in vivo correspond to sites phosphorylated in vitro by both p3pdcz and mitogen-activated protein (map) kinase. we have also shown that phosphorylation of ser1353 and ser1360 yields different phosphopeptide maps depending upon whether one or both of these sites are phosphorylated.
Identifier Residue Sequence Organism Cell Line
SIGNOR-30252 Ser1361 SPPKTKTsPKLSNKE Homo sapiens HeLa Cell
pmid sentence
We show that many of the sites phosphorylated on topoisomerase iia in vivo correspond to sites phosphorylated in vitro by both p3pdcz and mitogen-activated protein (map) kinase. we have also shown that phosphorylation of ser1353 and ser1360 yields different phosphopeptide maps depending upon whether one or both of these sites are phosphorylated.
Identifier Residue Sequence Organism Cell Line
SIGNOR-30256 Ser1393 GSVPLSSsPPATHFP Homo sapiens
pmid sentence
We show that many of the sites phosphorylated on topoisomerase iia in vivo correspond to sites phosphorylated in vitro by both p3pdcz and mitogen-activated protein (map) kinase. phosphopeptide 1 was eliminated by replacement of ser1392
Publications: 4 Organism: Homo Sapiens
+ PLK1up-regulates img/direct-activation.png phosphorylation TOP2A 0.491
Identifier Residue Sequence Organism Cell Line
SIGNOR-160233 Ser1337 LDSDEDFsDFDEKTD Homo sapiens
pmid sentence
Plk1 phosphorylates ser(1337) and ser(1524) of topoiialpha plk1-associated phosphorylation is essential for the functions of topoiialpha in mitosis
Identifier Residue Sequence Organism Cell Line
SIGNOR-182844 Ser1525 PIKYLEEsDEDDLF Homo sapiens
pmid sentence
Here we report that when phosphorylated, ser 1524 of topo iialpha acts as a binding site for the brct domain of mdc1 (mediator of dna damage checkpoint protein-1), thereby recruiting mdc1 to chromatin
Identifier Residue Sequence Organism Cell Line
SIGNOR-160237 Ser1525 PIKYLEEsDEDDLF Homo sapiens
pmid sentence
Plk1 phosphorylates ser(1337) and ser(1524) of topoiialpha plk1-associated phosphorylation is essential for the functions of topoiialpha in mitosis
Publications: 3 Organism: Homo Sapiens
+ GSK3Bdown-regulates quantity by destabilization img/direct_inhibition.png phosphorylation TOP2A 0.354
Identifier Residue Sequence Organism Cell Line
SIGNOR-276301 Ser1361 SPPKTKTsPKLSNKE Homo sapiens PLC-PRF-5 Cell
pmid sentence
 This study also reports the novel finding that topoIIα may be a target of GSK3β phosphorylation. Evidence suggests that CK2 serves as a priming kinase, through phosphorylation at Ser1365, for GSK3β-mediated phosphorylation at Ser1361.
Publications: 1 Organism: Homo Sapiens
+ CSNK2A1down-regulates quantity by destabilization img/direct_inhibition.png phosphorylation TOP2A 0.609
Identifier Residue Sequence Organism Cell Line
SIGNOR-276300 Ser1365 TKTSPKLsNKELKPQ Homo sapiens PLC-PRF-5 Cell
pmid sentence
 This study also reports the novel finding that topoIIα may be a target of GSK3β phosphorylation. Evidence suggests that CK2 serves as a priming kinase, through phosphorylation at Ser1365, for GSK3β-mediated phosphorylation at Ser1361.
Publications: 1 Organism: Homo Sapiens
+ CSNK2A1 img/unknown.png phosphorylation TOP2A 0.609
Identifier Residue Sequence Organism Cell Line
SIGNOR-250965 Ser1377 KPQKSVVsDLEADDV Homo sapiens HeLa Cell
pmid sentence
Tryptic phosphopeptide mapping revealed that casein kinase II phosphorylated the C-terminal domain primarily on 2 serine residues in vitro, which were shown to be sites of modification in vivo. Site-directed mutagenesis studies identified these casein kinase II-specific phosphorylation sites as serine 1524 and serine 1376.
Identifier Residue Sequence Organism Cell Line
SIGNOR-250966 Thr1343 FSDFDEKtDDEDFVP Homo sapiens
pmid sentence
Casein kinase II catalyzes a mitotic phosphorylation on threonine 1342 of human DNA topoisomerase IIalpha
Publications: 2 Organism: Homo Sapiens
+ CSNK2A1up-regulates img/direct-activation.png phosphorylation TOP2A 0.609
Identifier Residue Sequence Organism Cell Line
SIGNOR-182840 Ser1525 PIKYLEEsDEDDLF Homo sapiens
pmid sentence
Here we report that when phosphorylated, ser 1524 of topo iialpha acts as a binding site for the brct domain of mdc1 (mediator of dna damage checkpoint protein-1), thereby recruiting mdc1 to chromatin
Publications: 1 Organism: Homo Sapiens
+ PRKCBup-regulates activity img/direct-activation.png phosphorylation TOP2A 0.363
Identifier Residue Sequence Organism Cell Line
SIGNOR-249195 Ser29 EDAKKRLsVERIYQK Homo sapiens HeLa Cell
pmid sentence
Here, we have shown that the enzymatic activity of topoisomerase II alpha protein purified from HeLa cell nuclei was strongly enhanced following phosphorylation by protein kinase C. | Site-directed mutagenesis studies indicated that phosphorylation of serine 29 generated both of these phosphopeptides.
Publications: 1 Organism: Homo Sapiens
+ PRKCGup-regulates activity img/direct-activation.png phosphorylation TOP2A 0.363
Identifier Residue Sequence Organism Cell Line
SIGNOR-249196 Ser29 EDAKKRLsVERIYQK Homo sapiens HeLa Cell
pmid sentence
Here, we have shown that the enzymatic activity of topoisomerase II alpha protein purified from HeLa cell nuclei was strongly enhanced following phosphorylation by protein kinase C. | Site-directed mutagenesis studies indicated that phosphorylation of serine 29 generated both of these phosphopeptides.
Publications: 1 Organism: Homo Sapiens
+ PLK3up-regulates img/direct-activation.png phosphorylation TOP2A 0.271
Identifier Residue Sequence Organism Cell Line
SIGNOR-159596 Thr1343 FSDFDEKtDDEDFVP Homo sapiens
pmid sentence
The direct phosphorylation of thr(1342) of topoisomerase iialpha by plk3 was demonstrated with an in vitro kinase assay, and overexpression of plk3 induced the phosphorylation of thr(1342) in cellular topoisomerase iialpha. it is possible that plk3 regulates the activity of topoisomerase iia by phosphorylation in a cell-cycle dependent manner. Another possibility is that plk3 regulates the activity of topoisomerase iia when the checkpoint is activated.
Publications: 1 Organism: Homo Sapiens
+ SCF-FBW7down-regulates quantity by destabilization img/direct_inhibition.png polyubiquitination TOP2A 0.348
Identifier Residue Sequence Organism Cell Line
SIGNOR-276302 Homo sapiens PLC-PRF-5 Cell
pmid sentence
Evidence that Fbw7 acts as the E3-ligase mediating the degradation of topoIIα in HDAC inhibitor-treated PLC5 cells. 
Publications: 1 Organism: Homo Sapiens
+ YAP/TAZup-regulates quantity by expression img/indirect-activation.png transcriptional regulation TOP2A 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-276582
pmid sentence
By gene expression, exogenous YAP turns on its targets, but not in cells treated with JQ1 or depleted of BET-proteins (Fig. 3b and Supplementary Fig. 3e), indicating that BRD4 operates downstream of YAP/TAZ.
Publications: 1
+ idarubicindown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259327 Homo sapiens
pmid sentence
Topoisomerase II (Top2) is a nuclear enzyme involved in several metabolic processes of DNA. Chemotherapy agents that poison Top2 are known to induce persistent protein-mediated DNA double strand breaks (DSB). In this report, by using knock down experiments, we demonstrated that Top2α was largely responsible for the induction of γH2AX and cytotoxicity by the Top2 poisons idarubicin and etoposide in normal human cells.
Publications: 1 Organism: Homo Sapiens
+ NFYup-regulates quantity by expression img/direct-activation.png transcriptional regulation TOP2A 0.274
Identifier Residue Sequence Organism Cell Line
SIGNOR-242526 Homo sapiens
pmid sentence
The expression of human TOP2A is controlled by its promoter region that contains two GC boxes and five CCAAT boxes. NF-Y recognizes and binds to the ICBs. This binding of NF-Y to the TOP2A promoter can be promoted by HMGB1/2 and inhibited by pRb.
Publications: 1 Organism: Homo Sapiens
+ Doxorubicin hydrochloridedown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259324 Homo sapiens
pmid sentence
DNA topoisomerase II as the primary target of anti-tumor anthracyclines.Such studies have also given evidence of the peculiar features of the drug interference with DNA topoisomerase II activity. In contrast to other cytotoxic topoisomerase II inhibitors (acridines, epipodophyllotoxins), anthracyclines produce persistent DNA cleavable complexes. This property is more evident with doxorubicin derivatives than with daunorubicin derivatives.
Publications: 1 Organism: Homo Sapiens
+ doxorubicindown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-261911 Homo sapiens
pmid sentence
An important reason why Top2 has held the interest of researchers studying cancer was the discovery that active anti-cancer drugs, notably etoposide and doxorubicin target Top2
Publications: 1 Organism: Homo Sapiens
+ Daunorubicin hydrochloridedown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259322 Homo sapiens
pmid sentence
DNA topoisomerase II as the primary target of anti-tumor anthracyclines.Such studies have also given evidence of the peculiar features of the drug interference with DNA topoisomerase II activity. In contrast to other cytotoxic topoisomerase II inhibitors (acridines, epipodophyllotoxins), anthracyclines produce persistent DNA cleavable complexes. This property is more evident with doxorubicin derivatives than with daunorubicin derivatives.
Publications: 1 Organism: Homo Sapiens
+ 4'-epidoxorubicindown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259282 Homo sapiens Non-small Cell Lung Cancer Cell
pmid sentence
The combinatory use of low concentrations of SM with low-toxic topoisomerase II inhibitor epirubicin accelerated apoptotic cell death.
Publications: 1 Organism: Homo Sapiens
+ etoposidedown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259325 Homo sapiens
pmid sentence
Etoposide is an important chemotherapeutic agent that is used to treat a wide spectrum of human cancers. It has been in clinical use for more than two decades and remains one of the most highly prescribed anticancer drugs in the world. The primary cytotoxic target for etoposide is topoisomerase II.
Publications: 1 Organism: Homo Sapiens
+ TOP2Adown-regulates img/indirect_inhibition.png Survival 0.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-242537 Homo sapiens
pmid sentence
Down-regulation of DNA topoisomerase IIalpha leads to prolonged cell cycle transit in G2 and early M phases and increased survival to microtubule-interacting agents
Publications: 1 Organism: Homo Sapiens
+ valrubicindown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259383 Homo sapiens
pmid sentence
Valrubicin (N-trifluoroacetyladriamycin-14-valerate) is a semi-synthetic derivative of the anthracycline doxorubicin. Valrubicin inhibits the incorporation of nucleosides into nucleic acids, causing extensive chromosomal damage and cell-cycle arrest in the G2 phase. Its principal metabolites inhibit topoisomerase II, thus arresting DNA synthesis.
Publications: 1 Organism: Homo Sapiens
+ TOP2Aup-regulates img/indirect-activation.png Chromosome_segregation 0.7
Identifier Residue Sequence Organism Cell Line
SIGNOR-242530 Homo sapiens
pmid sentence
Topoisomerase IIalpha (topoIIalpha) is an essential mammalian enzyme that topologically modifies DNA and is required for chromosome segregation during mitosis.
Publications: 1 Organism: Homo Sapiens
+ YAP1up-regulates quantity by expression img/indirect-activation.png transcriptional regulation TOP2A 0.2
Identifier Residue Sequence Organism Cell Line
SIGNOR-276570
pmid sentence
By gene expression, exogenous YAP turns on its targets, but not in cells treated with JQ1 or depleted of BET-proteins (Fig. 3b and Supplementary Fig. 3e), indicating that BRD4 operates downstream of YAP/TAZ.
Publications: 1
Tissue: MCF-10A Cell
+ teniposidedown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-259329 Homo sapiens
pmid sentence
Recognition of transient DNA breaks induced by teniposide, etoposide, and other podophyllotoxin analogues established not only that their site of activity was DNA but also that their cytotoxic effect was dose-dependent. Extensive investigation has further indicated that a primary mechanism of action of these agents involves inhibition of the catalytic activity of eukaryote topoisomerase II and, more important, the consequent stabilization of the normally transient covalent intermediate formed between the DNA substrate and the enzyme.
Publications: 1 Organism: Homo Sapiens
+ 2-(Decan-2-ylamino)ethyl 4-aminobenzoatedown-regulates activity img/direct_inhibition.png chemical inhibition TOP2A 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-257768 Homo sapiens K-562 Cell
pmid sentence
As shown in Table 1 all of the bisanthrapyrazoles inhibited the decatenation activity of human topoisomerase IIα in the low micromolar concentration range
Publications: 1 Organism: Homo Sapiens
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