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DNA topoisomerase II alpha

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Target id: 2637

Nomenclature: DNA topoisomerase II alpha

Family: DNA topoisomerases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1531 17q21.2 TOP2A DNA topoisomerase II alpha
Mouse - 1528 11 62.91 cM Top2a topoisomerase (DNA) II alpha
Rat - 1526 10q31 Top2a DNA topoisomerase II alpha
Previous and Unofficial Names Click here for help
DNA topoisomerase 2-alpha | topoisomerase (DNA) II alpha | topoisomerase (DNA) II alpha 170kDa
Database Links Click here for help
Alphafold P11388 (Hs), Q01320 (Mm), P41516 (Rn)
BRENDA 5.99.1.2
CATH/Gene3D 3.30.565.10, 3.30.1360.40, 3.30.230.10, 1.10.268.10, 3.40.50.670, 3.90.199.10
ChEMBL Target CHEMBL1806 (Hs), CHEMBL3586 (Mm), CHEMBL3400 (Rn)
DrugBank Target P11388 (Hs)
Ensembl Gene ENSG00000131747 (Hs), ENSMUSG00000020914 (Mm), ENSRNOG00000053047 (Rn)
Entrez Gene 7153 (Hs), 21973 (Mm), 360243 (Rn)
Human Protein Atlas ENSG00000131747 (Hs)
KEGG Enzyme 5.99.1.2
KEGG Gene hsa:7153 (Hs), mmu:21973 (Mm), rno:360243 (Rn)
OMIM 126430 (Hs)
Orphanet ORPHA353516 (Hs)
Pharos P11388 (Hs)
RefSeq Nucleotide NM_001067 (Hs), NM_011623 (Mm), NM_022183 (Rn)
RefSeq Protein NP_001058 (Hs), NP_035753 (Mm), NP_071519 (Rn)
UniProtKB P11388 (Hs), Q01320 (Mm), P41516 (Rn)
Wikipedia TOP2A (Hs)
Enzyme Reaction Click here for help
EC Number: 5.99.1.2

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
etoposide Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 7.3 pIC50
⤷ pIC50 7.3 (IC50 5.04x10-8 M)
Description: Note: enzyme subunit is not specified in the referenced article
doxorubicin Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 6.0 pIC50 4
⤷ pIC50 6.0 (IC50 1x10-6 M) [4]
Description: In vitro inhibition of DNA relaxation and decatenation activities in a topoisomerase extract from human placenta.
mitoxantrone Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibition 5.3 pIC50 3
⤷ pIC50 5.3 (IC50 5.3x10-6 M) [3]
Description: Inhibition of topoisomerase IIα-mediated decatenation activity.
teniposide Small molecule or natural product Approved drug Ligand has a PDB structure Mm Inhibition - - 2
⤷ [2]
Description: Inhibition of purified mouse topoisomerase IIα, 170kDa isoform
View species-specific inhibitor tables
Immuno Process Associations
Immuno Process:  Immune system development
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Neuroblastoma
Disease Ontology: DOID:769
Orphanet: ORPHA635
References:  1

References

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1. Albino D, Scaruffi P, Moretti S, Coco S, Truini M, Di Cristofano C, Cavazzana A, Stigliani S, Bonassi S, Tonini GP. (2008) Identification of low intratumoral gene expression heterogeneity in neuroblastic tumors by genome-wide expression analysis and game theory. Cancer, 113 (6): 1412-22. [PMID:18671248]

2. Drake FH, Hofmann GA, Bartus HF, Mattern MR, Crooke ST, Mirabelli CK. (1989) Biochemical and pharmacological properties of p170 and p180 forms of topoisomerase II. Biochemistry, 28 (20): 8154-60. [PMID:2557897]

3. Hasinoff BB, Liang H, Wu X, Guziec LJ, Guziec Jr FS, Marshall K, Yalowich JC. (2008) The structure-based design, synthesis and biological evaluation of DNA-binding bisintercalating bisanthrapyrazole anticancer compounds. Bioorg Med Chem, 16 (7): 3959-68. [PMID:18258442]

4. Suzuki K, Yahara S, Maehata K, Uyeda M. (2001) Isoaurostatin, a novel topoisomerase inhibitor produced by Thermomonospora alba. J Nat Prod, 64 (2): 204-7. [PMID:11430001]

How to cite this page

DNA topoisomerases: DNA topoisomerase II alpha. Last modified on 18/08/2017. Accessed on 16/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=2637.