scholarly journals Exploration of the Role of the C-Terminal Domain of Human DNA Topoisomerase IIα in Catalytic Activity

ACS Omega ◽  
2021 ◽  
Vol 6 (40) ◽  
pp. 25892-25903
Author(s):  
Ashley C. Dougherty ◽  
Mariam G. Hawaz ◽  
Kristine G. Hoang ◽  
Judy Trac ◽  
Jacob M. Keck ◽  
...  
Keyword(s):  
Catalytic Activity ◽  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Terminal Domain ◽  
Human Dna ◽  
Dna Topoisomerase Iiα

scholarly journals The Role of an Inverted CCAAT Element in Transcriptional Activation of the Human DNA Topoisomerase IIα Gene by Heat Shock

1998 ◽  
Vol 273 (17) ◽  
pp. 10550-10555 ◽  
Author(s):  
Manabu Furukawa ◽  
Takeshi Uchiumi ◽  
Minoru Nomoto ◽  
Hiroshi Takano ◽  
Richard I. Morimoto ◽  
...  
Keyword(s):  
Heat Shock ◽  
Transcriptional Activation ◽  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Dna Topoisomerase Iiα

scholarly journals Probing Conformational Changes in Human DNA Topoisomerase IIα by Pulsed Alkylation Mass Spectrometry

2012 ◽  
Vol 287 (30) ◽  
pp. 25660-25668 ◽  
Author(s):  
Yu-tsung Chen ◽  
Tammy R. L. Collins ◽  
Ziqiang Guan ◽  
Vincent B. Chen ◽  
Tao-Shih Hsieh
Keyword(s):  
Mass Spectrometry ◽  
Conformational Changes ◽  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Dna Topoisomerase Iiα

Discovery of new ATP-competitive inhibitors of human DNA topoisomerase IIα through screening of bacterial topoisomerase inhibitors

2020 ◽  
Vol 102 ◽  
pp. 104049
Author(s):  
Žiga Skok ◽  
Martina Durcik ◽  
Darja Gramec Skledar ◽  
Michaela Barančoková ◽  
Lucija Peterlin Mašič ◽  
...  
Keyword(s):  
Topoisomerase Inhibitors ◽  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Competitive Inhibitors ◽  
Dna Topoisomerase Iiα

4,6-Substituted-1,3,5-triazin-2(1H)-ones as monocyclic catalytic inhibitors of human DNA topoisomerase IIα targeting the ATP binding site

2015 ◽  
Vol 23 (15) ◽  
pp. 4218-4229 ◽  
Author(s):  
Barbara Pogorelčnik ◽  
Matej Janežič ◽  
Izidor Sosič ◽  
Stanislav Gobec ◽  
Tom Solmajer ◽  
...  
Keyword(s):  
Binding Site ◽  
Atp Binding ◽  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Atp Binding Site ◽  
Human Dna ◽  
Dna Topoisomerase Iiα

scholarly journals Substituted 4,5′-Bithiazoles as Catalytic Inhibitors of Human DNA Topoisomerase IIα

2020 ◽  
Vol 60 (7) ◽  
pp. 3662-3678
Author(s):  
Kaja Bergant Loboda ◽  
Matej Janežič ◽  
Martina Štampar ◽  
Bojana Žegura ◽  
Metka Filipič ◽  
...  
Keyword(s):  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Dna Topoisomerase Iiα

Bioassays and In Silico Methods in the Identification of Human DNA Topoisomerase IIα Inhibitors

2018 ◽  
Vol 25 (28) ◽  
pp. 3286-3318 ◽  
Author(s):  
Kaja Bergant ◽  
Matej Janezic ◽  
Andrej Perdih
Keyword(s):  
In Silico ◽  
In Vivo Studies ◽  
Topoisomerase Iiα ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Practical Guidelines ◽  
In Silico Methods ◽  
Dna Topoisomerase Iiα

Background: The family of DNA topoisomerases comprises a group of enzymes that catalyse the induction of topological changes to DNA. These enzymes play a role in the cell replication machinery and are, therefore, important targets for anticancer drugs - with human DNA topoisomerase IIα being one of the most prominent. Active compounds targeting this enzyme are classified into two groups with diverse mechanisms of action: DNA poisons act by stabilizing a covalent cleavage complex between DNA and the topoisomerase enzyme, transforming it into a cellular toxin, while the second diverse group of catalytic inhibitors, provides novel inhibition avenues for tackling this enzyme due to frequent occurrence of side effects observed during the DNA poison therapy. Methods: Based on a comprehensive literature search we present an overview of available bioassays and in silico methods in the identification of human DNA topoisomerase IIα inhibitors. Results and Conclusion: A comprehensive outline of the available methods and approaches that explore in detail the in vitro mechanistic and functional aspects of the topoisomerase IIα inhibition of both topo IIα inhibitor groups is presented. The utilized in vitro cell-based assays and in vivo studies to further explore the validated topo IIα inhibitors in subsequent preclinical stages of the drug discovery are discussed. The potential of in silico methods in topoisomerase IIα inhibitor discovery is outlined. A list of practical guidelines was compiled to aid new as well experienced researchers in how to optimally approach the design of targeted inhibitors and validation in the preclinical drug development stages.

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