Nitrosourea Derivatives of 3',4'-Didemethoxy-3',4'-dioxo-4-deoxypodophyllotoxin and Urea Derivatives of 4'-O-Demethylpodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase

Heterocycles ◽  
1994 ◽  
Vol 39 (1) ◽  
pp. 361 ◽  
Author(s):  
Kuo-Hsiung Lee ◽  
Makoto Miyahara ◽  
Yoshiki Kashiwada ◽  
Xin Guo ◽  
Hong-Xing Chen ◽  
...  
Keyword(s):  
Dna Topoisomerase ◽  
Urea Derivatives ◽  
Human Dna ◽  
Derivatives Of

Inhibition of Human DNA Topoisomerase I by New DNA Minor Groove Ligands: Derivatives of Oligo-1,3-Thiazolecarboxamides

2001 ◽  
Vol 11 (3) ◽  
pp. 137-147 ◽  
Author(s):  
Dmitry V. Bugreev ◽  
Elena L. Vasyutina ◽  
Vladimir A. Ryabinin ◽  
Alexander N. Sinyakov ◽  
Valentina N. Buneva ◽  
...  
Keyword(s):  
Topoisomerase I ◽  
Minor Groove ◽  
Dna Topoisomerase I ◽  
Dna Topoisomerase ◽  
Dna Minor Groove ◽  
Human Dna ◽  
Derivatives Of ◽  
Human Dna Topoisomerase I

Antitumor agents. 100. Inhibition of human DNA topoisomerase II by cytotoxic ether and ester derivatives of podophyllotoxin and .alpha.-peltatin

1989 ◽  
Vol 32 (3) ◽  
pp. 604-608 ◽  
Author(s):  
Lee S. Thurston ◽  
Yasuhiro Imakura ◽  
Mitsumasa Haruna ◽  
De Hua Li ◽  
Zong Chao Liu ◽  
...  
Keyword(s):  
Topoisomerase Ii ◽  
Antitumor Agents ◽  
Dna Topoisomerase Ii ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Derivatives Of

scholarly journals In Vitro and In Silico Characterization of an Antimalarial Compound with Antitumor Activity Targeting Human DNA Topoisomerase IB

2021 ◽  
Vol 22 (14) ◽  
pp. 7455
Author(s):  
Bini Chhetri Soren ◽  
Jagadish Babu Dasari ◽  
Alessio Ottaviani ◽  
Beatrice Messina ◽  
Giada Andreotti ◽  
...  
Keyword(s):  
Enzyme Reaction ◽  
Dna Topoisomerase ◽  
Human Dna ◽  
Topoisomerase Ib ◽  
Topological State ◽  
Cleavage Step ◽  
Dynamics Simulations ◽  
In Silico Characterization ◽  
Dna Complex

Human DNA topoisomerase IB controls the topological state of supercoiled DNA through a complex catalytic cycle that consists of cleavage and religation reactions, allowing the progression of fundamental DNA metabolism. The catalytic steps of human DNA topoisomerase IB were analyzed in the presence of a drug, obtained by the open-access drug bank Medicines for Malaria Venture. The experiments indicate that the compound strongly and irreversibly inhibits the cleavage step of the enzyme reaction and reduces the cell viability of three different cancer cell lines. Molecular docking and molecular dynamics simulations suggest that the drug binds to the human DNA topoisomerase IB-DNA complex sitting inside the catalytic site of the enzyme, providing a molecular explanation for the cleavage-inhibition effect. For all these reasons, the aforementioned drug could be a possible lead compound for the development of an efficient anti-tumor molecule targeting human DNA topoisomerase IB.

103 Site-directed mutagenesis of human DNA topoisomerase IIβ

1997 ◽  
Vol 25 (4) ◽  
pp. S638-S638 ◽  
Author(s):  
KATHERINE L. MARSH ◽  
EMMA L. MECZES ◽  
RONALD THORN ◽  
RICHARD MARSHALL ◽  
CAROLINE A. AUSTIN
Keyword(s):  
Site Directed Mutagenesis ◽  
Directed Mutagenesis ◽  
Dna Topoisomerase ◽  
Human Dna
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