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DNA topoisomerase I

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Target not currently curated in GtoImmuPdb

Target id: 2636

Nomenclature: DNA topoisomerase I

Family: DNA topoisomerases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 765 20q12 TOP1 DNA topoisomerase I
Mouse - 767 2 80.96 cM Top1 topoisomerase (DNA) I
Rat - 767 3q42 Top1 DNA topoisomerase I
Previous and Unofficial Names Click here for help
topoisomerase (DNA) I
Database Links Click here for help
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
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RefSeq Nucleotide
RefSeq Protein
UniProtKB
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Enzyme Reaction Click here for help
EC Number: 5.99.1.2

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 5z [PMID: 8410981] Small molecule or natural product Bt Inhibition 7.6 pIC50 5
pIC50 7.6 (IC50 2.7x10-8 M) [5]
Description: Inhibition of pBR322 DNA cleavage by calf thymus DNA topoisomerase I.
compound 19 [PMID: 7707314] Small molecule or natural product Bt Inhibition 7.6 pIC50 4
pIC50 7.6 (IC50 2.8x10-8 M) [4]
Description: Concentration of compound required to produce approximately 50% fragmentation of P-32 end- labeled DNA in the presence of calf thymus topoisomerase I.
irinotecan Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Bt Inhibition - - 1,3
[1,3]
Description: Effect of irinotecan on topoisomerase I-mediated DNA cleavage
(S)-DRF-1042 Small molecule or natural product Primary target of this compound Hs Inhibition - - 2
[2]
View species-specific inhibitor tables

References

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1. Dodds HM, Haaz MC, Riou JF, Robert J, Rivory LP. (1998) Identification of a new metabolite of CPT-11 (irinotecan): pharmacological properties and activation to SN-38. J Pharmacol Exp Ther, 286 (1): 578-83. [PMID:9655905]

2. Nekkanti VK, Karatgi PJ, Paithankar M, Pillai RS, Venkateswarlu A, Shanvas A, Kumar RA, Ramesh M, Raju S, Subrahmanyam D et al.. (2011) Pharmaceutical compositions of [5(s)-(2'-hydroxyethoxy)-20(s)-camptothecin. Patent number: US20110177161. Assignee: Dr. Reddy's Laboratories Limited,. Priority date: 24/05/2007. Publication date: 21/07/2011.

3. Tanizawa A, Fujimori A, Fujimori Y, Pommier Y. (1994) Comparison of topoisomerase I inhibition, DNA damage, and cytotoxicity of camptothecin derivatives presently in clinical trials. J Natl Cancer Inst, 86 (11): 836-42. [PMID:8182764]

4. Uehling DE, Nanthakumar SS, Croom D, Emerson DL, Leitner PP, Luzzio MJ, McIntyre G, Morton B, Profeta S, Sisco J et al.. (1995) Synthesis, topoisomerase I inhibitory activity, and in vivo evaluation of 11-azacamptothecin analogs. J Med Chem, 38 (7): 1106-18. [PMID:7707314]

5. Wall ME, Wani MC, Nicholas AW, Manikumar G, Tele C, Moore L, Truesdale A, Leitner P, Besterman JM. (1993) Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs. J Med Chem, 36 (18): 2689-700. [PMID:8410981]

How to cite this page

DNA topoisomerases: DNA topoisomerase I. Last modified on 18/08/2017. Accessed on 05/08/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2636.