scholarly journals A T5 Exonuclease-Based Assay for DNA Topoisomerases and DNA Intercalators

ACS Omega ◽  
2021 ◽  
Author(s):  
Zifang Deng ◽  
Fenfei Leng
Keyword(s):  
Dna Topoisomerases ◽  
Dna Intercalators

Hybrid Imidazole-Pyridine Derivatives: An Approach to Novel Anticancer DNA Intercalators

2020 ◽  
Vol 27 (1) ◽  
pp. 154-169 ◽  
Author(s):  
Claudiu N. Lungu ◽  
Bogdan Ionel Bratanovici ◽  
Maria Mirabela Grigore ◽  
Vasilichia Antoci ◽  
Ionel I. Mangalagiu
Keyword(s):  
Experimental Data ◽  
Antimicrobial Properties ◽  
Qsar Model ◽  
Therapeutic Effectiveness ◽  
Computational Results ◽  
Pyridine Derivatives ◽  
Quadruplex Dna ◽  
Dna Intercalators ◽  
Structure Activity ◽  
G Quadruplex

Lack of specificity and subsequent therapeutic effectiveness of antimicrobial and antitumoral drugs is a common difficulty in therapy. The aim of this study is to investigate, both by experimental and computational methods, the antitumoral and antimicrobial properties of a series of synthesized imidazole-pyridine derivatives. Interaction with three targets was discussed: Dickerson-Drew dodecamer (PDB id 2ADU), G-quadruplex DNA string (PDB id 2F8U) and DNA strain in complex with dioxygenase (PDB id 3S5A). Docking energies were computed and represented graphically. On them, a QSAR model was developed in order to further investigate the structure-activity relationship. Results showed that synthesized compounds have antitumoral and antimicrobial properties. Computational results agreed with the experimental data.

DNA Topoisomerases as Targets for Antiprotozoal Therapy

2003 ◽  
Vol 3 (6) ◽  
pp. 597-608 ◽  
Author(s):  
R. Bakshi ◽  
T. Shapiro
Keyword(s):  
Dna Topoisomerases

Inhibition of DNA Topoisomerases by a Series of Benzoxazoles and their Possible Metabolites

2018 ◽  
Vol 15 (11) ◽  
pp. 1155-1162
Author(s):  
Fatma Zilifdar ◽  
Egemen Foto ◽  
Tugba Ertan-Bolelli ◽  
Ilkay Yildiz ◽  
Esin Aki-Yalcin ◽  
...  
Keyword(s):  
Dna Topoisomerases

Antitumor Effect of Pomolic Acid in Acute Myeloid Leukemia Cells Involves Cell Death, Decreased Cell Growth and Topoisomerases Inhibition

2019 ◽  
Vol 18 (10) ◽  
pp. 1457-1468
Author(s):  
Michelle X.G. Pereira ◽  
Amanda S.O. Hammes ◽  
Flavia C. Vasconcelos ◽  
Aline R. Pozzo ◽  
Thaís H. Pereira ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Death ◽  
Acute Myeloid Leukemia ◽  
Cell Lines ◽  
Myeloid Leukemia ◽  
Natural Compound ◽  
Dna Topoisomerases ◽  
Human Dna ◽  
Pomolic Acid ◽  
Acute Myeloid

Background: Acute myeloid leukemia (AML) represents the largest number of annual deaths from hematologic malignancy. In the United States, it was estimated that 21.380 individuals would be diagnosed with AML and 49.5% of patients would die in 2017. Therefore, the search for novel compounds capable of increasing the overall survival rate to the treatment of AML cells is urgent. Objectives: To investigate the cytotoxicity effect of the natural compound pomolic acid (PA) and to explore the mechanism of action of PA in AML cell lines with different phenotypes. Methods: Three different AML cell lines, HL60, U937 and Kasumi-1 cells with different mechanisms of resistance were used to analyze the effect of PA on the cell cycle progression, on DNA intercalation and on human DNA topoisomerases (hTopo I and IIα) in vitro studies. Theoretical experiments of the inhibition of hTopo I and IIα were done to explore the binding modes of PA. Results: PA reduced cell viability, induced cell death, increased sub-G0/G1 accumulation and activated caspases pathway in all cell lines, altered the cell cycle distribution and inhibited the catalytic activity of both human DNA topoisomerases. Conclusion: Finally, this study showed that PA has powerful antitumor activity against AML cells, suggesting that this natural compound might be a potent antineoplastic agent to improve the treatment scheme of this neoplasm.

Discovery of novel triazolophthalazine derivatives as DNA intercalators and topoisomerase II inhibitors

2021 ◽  
Author(s):  
Helmy Sakr ◽  
Rezk R. Ayyad ◽  
Ali A. El‐Helby ◽  
Mohamed M. Khalifa ◽  
Hazem A. Mahdy
Keyword(s):  
Topoisomerase Ii ◽  
Dna Intercalators ◽  
Topoisomerase Ii Inhibitors

scholarly journals DNA topoisomerases: why so many?

1991 ◽  
Vol 266 (11) ◽  
pp. 6659-6662
Author(s):  
J C Wang
Keyword(s):  
Dna Topoisomerases

scholarly journals Developmental Regulation of DNA-Topoisomerases during Drosophila Embryogenesis

2001 ◽  
Vol 262 (2) ◽  
pp. 114-121 ◽  
Author(s):  
Mark J. Gemkow ◽  
Joachim Dichter ◽  
Donna J. Arndt-Jovin
Keyword(s):  
Developmental Regulation ◽  
Dna Topoisomerases ◽  
Drosophila Embryogenesis
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