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50 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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TOP2A
DNA topoisomerase II alpha
Chromosome 17 · 17q21.2
NCBI Gene: 7153Ensembl: ENSG00000131747.16HGNC: HGNC:11989UniProt: P11388
681PubMed Papers
20Diseases
26Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Hub Gene
RESEARCH IMPACT
Highly StudiedTrending
CLINICAL
FDA Approved Target
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
nucleolusnuclear chromosomecentriolemagnesium ion bindingneoplasmbreast canceracute myeloid leukemiamultiple myeloma
✦AI Summary

TOP2A (DNA topoisomerase II alpha) is a critical enzyme that resolves DNA topological stress by creating transient double-stranded breaks, passing intact DNA strands through the break, and religating the DNA 1. This decatenating activity is essential for DNA replication and transcription, particularly under high-output conditions 1. TOP2A functions as part of MYC-assembled 'topoisome' complexes that enhance topoisomerase activity at promoters and enhancers 1. Dysregulated TOP2A expression is associated with multiple malignancies including hepatocellular carcinoma, breast, prostate, colon, and lung cancers 2. TOP2A gene amplification occurs frequently adjacent to HER-2 in breast tumors and correlates with both chemotherapy sensitivity and resistance depending on copy number status 3. Elevated TOP2A expression promotes tumor progression and chemotherapy resistance; for example, in nasopharyngeal carcinoma, the USP7/KDM5B/ZBTB16/TOP2A axis regulates cisplatin resistance 4. In hepatocellular carcinoma, EZH2-mediated epigenetic silencing of miR-139-5p increases TOP2A expression, inhibiting cellular senescence 5. Clinically, TOP2A amplification predicts anthracycline chemotherapy response, yet overexpression indicates poor prognosis and disease recurrence risk 2. TOP2A deficiency impairs trophoblast function and embryonic development, linking it to recurrent spontaneous abortion 6. These findings establish TOP2A as a key prognostic biomarker and therapeutic target across multiple cancer types.

Sources cited
1
TOP2A functions to resolve DNA topological stress and is assembled into MYC-nucleated complexes that stimulate topoisomerase activity
PMID: 34890565
2
TOP2A is dysregulated in various malignancies and increased expression correlates with poor clinical outcomes and reduced survival
PMID: 39454521
3
TOP2A gene amplification and deletion occur frequently near HER-2 in breast cancer and influence chemotherapy sensitivity/resistance
PMID: 14632727
4
TOP2A expression is regulated by the USP7/KDM5B/ZBTB16 axis and mediates cisplatin resistance in nasopharyngeal carcinoma
PMID: 38287116
5
EZH2-mediated H3K27me3 silencing of miR-139-5p increases TOP2A expression and inhibits cellular senescence in hepatocellular carcinoma
PMID: 38008711
6
TOP2A deficiency impairs trophoblast proliferation, migration, and invasion through FOXO pathway activation and is associated with recurrent spontaneous abortion
PMID: 36585615
Disease Associationsⓘ20
neoplasmOpen Targets
0.62Moderate
breast cancerOpen Targets
0.61Moderate
acute myeloid leukemiaOpen Targets
0.60Moderate
multiple myelomaOpen Targets
0.59Moderate
breast neoplasmOpen Targets
0.58Moderate
small cell lung carcinomaOpen Targets
0.58Moderate
Hodgkins lymphomaOpen Targets
0.57Moderate
sarcomaOpen Targets
0.56Moderate
Kaposi's sarcomaOpen Targets
0.56Moderate
ovarian neoplasmOpen Targets
0.55Moderate
ovarian cancerOpen Targets
0.55Moderate
lung cancerOpen Targets
0.54Moderate
urinary bladder carcinomaOpen Targets
0.53Moderate
prostate cancerOpen Targets
0.53Moderate
cancerOpen Targets
0.52Moderate
non-Hodgkins lymphomaOpen Targets
0.52Moderate
endometrial cancerOpen Targets
0.51Moderate
acute myelomonocytic leukemiaOpen Targets
0.50Moderate
acute myeloid leukemia by FAB classificationOpen Targets
0.49Moderate
breast carcinomaOpen Targets
0.49Moderate
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets26
ALDOXORUBICINPhase III
DNA topoisomerase II alpha inhibitor
soft tissue sarcoma
AMRUBICINApproved
DNA topoisomerase II alpha inhibitor
neoplasm
AMRUBICIN HYDROCHLORIDEPhase III
DNA topoisomerase II alpha inhibitor
small cell lung carcinoma
AMSACRINEApproved
DNA topoisomerase II inhibitor
BECATECARINPhase III
DNA topoisomerase I inhibitor
BERUBICINPhase II
DNA topoisomerase II inhibitor
BERUBICIN HYDROCHLORIDEPhase II
DNA topoisomerase II inhibitor
C-1311Phase II
DNA topoisomerase II inhibitor
breast cancer
DAUNORUBICINApproved
DNA topoisomerase II alpha inhibitor
acute myeloid leukemia by FAB classification
DAUNORUBICIN CITRATEPhase I
DNA topoisomerase II alpha inhibitor
breast cancer
DAUNORUBICIN HYDROCHLORIDEApproved
DNA topoisomerase II alpha inhibitor
DEXRAZOXANEApproved
DNA topoisomerase II inhibitor
breast cancer
DEXRAZOXANE HYDROCHLORIDEApproved
DNA topoisomerase II inhibitor
cardiomyopathy
DOXORUBICINApproved
DNA topoisomerase II alpha inhibitor
DOXORUBICIN HYDROCHLORIDEApproved
DNA topoisomerase II alpha inhibitor
bone sarcoma
ETOPOSIDEApproved
DNA topoisomerase II inhibitor
neoplasm
ETOPOSIDE PHOSPHATEPhase III
DNA topoisomerase II alpha inhibitor
lymphoma
GANCOTAMABPhase II/III
DNA topoisomerase II alpha inhibitor
breast cancer
IDARUBICINApproved
DNA topoisomerase II alpha inhibitor
acute myeloid leukemia by FAB classification
IDARUBICIN HYDROCHLORIDEApproved
DNA topoisomerase II alpha inhibitor
acute myeloid leukemia
MITOXANTRONEApproved
DNA topoisomerase II alpha inhibitor
MITOXANTRONE HYDROCHLORIDEApproved
DNA topoisomerase II alpha inhibitor
PAZUFLOXACINApproved
Bacterial DNA gyrase inhibitor
streptococcal pneumonia
TENIPOSIDEApproved
DNA topoisomerase II inhibitor
VALRUBICINApproved
DNA topoisomerase II alpha inhibitor
urinary bladder carcinoma
VOSAROXINApproved
DNA topoisomerase II inhibitor
neoplasm
Related Genes
TPX2Protein interaction100%PLK1Protein interaction100%CDC20Protein interaction100%KPNA2Protein interaction99%ESPL1Protein interaction99%CCNB2Protein interaction99%
Tissue Expression6 tissues
Brain
100%
Bone Marrow
51%
Lung
2%
Heart
1%
Liver
0%
Ovary
0%
Gene Interaction Network
Click a node to explore
TOP2ATPX2PLK1CDC20KPNA2ESPL1CCNB2
PROTEIN STRUCTURE
Preparing viewer…
PDB5NNE · 1.15 Å · X-ray
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
0.42Moderately Constrained
pLIⓘ
1.00Intolerant
Observed/Expected LoF0.33 [0.27–0.42]
RankingsWhere TOP2A stands among ~20K protein-coding genes
  • #320of 20,598
    Most Researched681 · top 5%
  • #87of 1,025
    FDA-Approved Drug Targets17 · top 10%
  • #2,237of 17,882
    Most Constrained (LOEUF)0.42 · top quartile
Genes detectedTOP2A
Sources retrieved50 papers
Response time—
📄 Sources
50▼
1
Genetic screens in human cells using the CRISPR-Cas9 system.
PMID: 24336569
Science · 2014
1.00
2
Type II topoisomerases shape multi-scale 3D chromatin folding in regions of positive supercoils.
PMID: 39486417
Mol Cell · 2024
0.92
3
Deubiquitinase USP7 stabilizes KDM5B and promotes tumor progression and cisplatin resistance in nasopharyngeal carcinoma through the ZBTB16/TOP2A axis.
PMID: 38287116
Cell Death Differ · 2024
0.90
4
HER2 and TOP2A Gene Amplification and Protein Expression in Upper Tract Urothelial Carcinomas.
PMID: 28755093
Pathol Oncol Res · 2018
0.82
5
Chromatin damage generated by DNA intercalators leads to degradation of RNA Polymerase II.
PMID: 38340348
Nucleic Acids Res · 2024
0.80