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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
DNA topoisomerases regulate the supercoiling of nuclear DNA to influence the capacity for replication or transcription. The enzymatic function of this series of enzymes involves cutting the DNA to allow unwinding, followed by re-attachment to reseal the backbone. Members of the family are targetted in anti-cancer chemotherapy.
* Key recommended reading is highlighted with an asterisk
Alagoz M, Gilbert DC, El-Khamisy S, Chalmers AJ. (2012) DNA repair and resistance to topoisomerase I inhibitors: mechanisms, biomarkers and therapeutic targets. Curr. Med. Chem., 19 (23): 3874-85. [PMID:22788763]
Baranello L, Kouzine F, Levens D. (2013) DNA Topoisomerases: Beyond the standard role. Transcription, 4 (5) [Epub ahead of print]. [PMID:24135702]
* Castelli S, Coletta A, D'Annessa I, Fiorani P, Tesauro C, Desideri A. (2012) Interaction between natural compounds and human topoisomerase I. Biol. Chem., 393 (11): 1327-40. [PMID:23109546]
Champoux JJ. (2001) DNA topoisomerases: structure, function, and mechanism. Annu. Rev. Biochem., 70: 369-413. [PMID:11395412]
* Chen SH, Chan NL, Hsieh TS. (2013) New mechanistic and functional insights into DNA topoisomerases. Annu. Rev. Biochem., 82: 139-70. [PMID:23495937]
Gilbert DC, Chalmers AJ, El-Khamisy SF. (2012) Topoisomerase I inhibition in colorectal cancer: biomarkers and therapeutic targets. Br. J. Cancer, 106 (1): 18-24. [PMID:22108516]
* Kathiravan MK, Khilare MM, Nikoomanesh K, Chothe AS, Jain KS. (2013) Topoisomerase as target for antibacterial and anticancer drug discovery. J Enzyme Inhib Med Chem, 28 (3): 419-35. [PMID:22380774]
* Tomicic MT, Kaina B. (2013) Topoisomerase degradation, DSB repair, p53 and IAPs in cancer cell resistance to camptothecin-like topoisomerase I inhibitors. Biochim. Biophys. Acta, 1835 (1): 11-27. [PMID:23006513]
Węsierska-Gądek J, Składanowski A. (2012) Therapeutic intervention by the simultaneous inhibition of DNA repair and type I or type II DNA topoisomerases: one strategy, many outcomes. Future Med Chem, 4 (1): 51-72. [PMID:22168164]
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. 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. 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]
Database page citation:
18.104.22.168 DNA Topoisomerases. Accessed on 27/03/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=851.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol. 172: 6024-6109.