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]

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