DNA topoisomerase I

Target id: 2636

Nomenclature: DNA topoisomerase I

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 I in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 765 20q12-q13.1 TOP1 DNA topoisomerase I
Mouse - 767 2 H2-3 Top1 topoisomerase (DNA) I
Rat - 767 3q42 Top1 topoisomerase (DNA) I
Previous and Unofficial Names
topoisomerase (DNA) I
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
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
compound 5z [PMID: 8410981] 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] 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 Bt Inhibition - - 1,3
[1,3]
Description: Effect of irinotecan on topoisomerase I-mediated DNA cleavage
(S)-DRF-1042 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

5.99.1.2 DNA Topoisomerases: DNA topoisomerase I. Last modified on 18/08/2017. Accessed on 19/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2636.