DNA topoisomerase II alpha

Target id: 2637

Nomenclature: DNA topoisomerase II alpha

Family: 5.99.1.2 DNA Topoisomerases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: OFF :     Currently no data for DNA topoisomerase II alpha in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1531 17q21-q22 TOP2A DNA topoisomerase II alpha
Mouse - 1528 11 D Top2a topoisomerase (DNA) II alpha
Rat - 1526 10q31 Top2a DNA topoisomerase II alpha
Previous and Unofficial Names
DNA topoisomerase 2-alpha | topoisomerase (DNA) II alpha | topoisomerase (DNA) II alpha 170kDa
Database Links
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Enzyme Reaction
EC Number: 5.99.1.2

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
etoposide 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 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 Hs Inhibition 5.3 pIC50 3
pIC50 5.3 (IC50 5.3x10-6 M) [3]
Description: Inhibition of topoisomerase IIα-mediated decatenation activity.
teniposide Mm Inhibition - - 2
[2]
Description: Inhibition of purified mouse topoisomerase IIα, 170kDa isoform
View species-specific inhibitor tables
Clinically-Relevant Mutations and Pathophysiology
Disease:  Neuroblastoma
Disease Ontology: DOID:769
Orphanet: ORPHA635
References:  1

References

Show »

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. Cancer113 (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. Biochemistry28 (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

5.99.1.2 DNA Topoisomerases: DNA topoisomerase II alpha. Last modified on 18/08/2017. Accessed on 16/12/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2637.