Page last updated: 2024-10-24

DNA topoisomerase binding

Definition

Target type: molecularfunction

Binding to a DNA topoisomerase. [GOC:jl]

DNA topoisomerases are enzymes that regulate the topological state of DNA by introducing transient breaks in the phosphodiester backbone. This allows the DNA to unwind or rewind, relieving torsional stress and facilitating processes like DNA replication, transcription, and recombination. The binding of a topoisomerase to DNA involves a multi-step process. First, the enzyme recognizes and binds to specific DNA sequences or structural features. This binding may involve interactions with the sugar-phosphate backbone, the bases, or both. Once bound, the topoisomerase then cleaves one or both strands of the DNA duplex, forming a transient covalent linkage between the enzyme and the DNA. This allows the DNA to rotate around the remaining intact strand, relieving topological constraints. Finally, the enzyme reseals the break, restoring the integrity of the DNA molecule. The precise mechanism of topoisomerase binding and cleavage varies depending on the specific enzyme and its cellular function. For example, type I topoisomerases cleave only one strand of DNA, while type II topoisomerases cleave both strands. The specific DNA sequences or structures recognized by topoisomerases also vary, influencing their role in different cellular processes. The regulation of topoisomerase activity is crucial for maintaining genomic integrity and cellular function. Dysregulation of these enzymes can lead to DNA damage, genomic instability, and disease. Therefore, understanding the molecular function of topoisomerase binding is essential for comprehending fundamental cellular processes and developing novel therapeutic strategies for treating various diseases.'
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Proteins (1)

ProteinDefinitionTaxonomy
Histone-lysine N-methyltransferase SETMARA histone-lysine N-methyltransferase SETMAR that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q53H47]Homo sapiens (human)

Compounds (1)

CompoundDefinitionClassesRoles
gsk343GSK343 : A member of the class of indazoles that is 1-isopropyl-1H-indazole-4-carboxamide in which the nitrogen of the carboxamide group is substituted by a (6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl group and in which the indazole ring is substituted at position 6 by a 2-(4-methylpiperazin-1-yl)pyridin-4-yl group. A highly potent and selective EZH2 inhibitor (IC50 = 4 nM).

GSK343: an EZH2 methyltransferase inhibitor
aminopyridine;
indazoles;
N-alkylpiperazine;
N-arylpiperazine;
pyridone;
secondary carboxamide
antineoplastic agent;
apoptosis inducer;
EC 2.1.1.43 (enhancer of zeste homolog 2) inhibitor