positive regulation of DNA topoisomerase (ATP-hydrolyzing) activity
Definition
Target type: biologicalprocess
Any process that activates or increases the frequency, rate or extent of DNA topoisomerase (ATP-hydrolyzing) activity. [GOC:mah]
Positive regulation of DNA topoisomerase (ATP-hydrolyzing) activity refers to the control mechanisms that enhance the enzymatic activity of DNA topoisomerases. These enzymes play a crucial role in managing the topological complexity of DNA, which arises from its double-stranded helical structure. DNA topoisomerases function by introducing transient breaks in the DNA backbone, allowing the strands to pass through one another, and then resealing the breaks. This process is essential for numerous cellular processes, including DNA replication, transcription, and recombination. Positive regulation of topoisomerase activity ensures that the enzyme is present and active when and where needed.
This regulation can occur at multiple levels, including:
* **Transcriptional regulation:** Genes encoding topoisomerases can be regulated at the transcriptional level, influencing the amount of enzyme produced. This can be controlled by various factors, such as growth factors, stress signals, or developmental cues.
* **Post-translational modifications:** Topoisomerases can be modified after translation, such as phosphorylation or acetylation, which can alter their activity. These modifications can be triggered by specific signaling pathways, affecting the enzyme's stability, localization, or interaction with other proteins.
* **Protein-protein interactions:** Topoisomerases can interact with other proteins that regulate their activity. These interactions can either stimulate or inhibit the enzyme's function. For example, some proteins can act as chaperones, assisting in topoisomerase folding or stability, while others may directly bind to the active site, influencing the enzyme's catalytic activity.
* **Small molecule interactions:** Topoisomerases can be targeted by small molecules, including drugs that can either inhibit or enhance their activity. These drugs are often used in the treatment of cancer, exploiting the dependence of tumor cells on topoisomerase activity for their rapid proliferation.
Overall, the positive regulation of DNA topoisomerase activity ensures that the enzyme is present and active at the appropriate time and location, allowing for proper DNA metabolism and the maintenance of genome integrity.'
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Proteins (2)
| Protein | Definition | Taxonomy |
|---|---|---|
| E3 ubiquitin-protein ligase UHRF1 | An E3 ubiquitin-protein ligase UHRF1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q96T88] | Homo sapiens (human) |
| Histone-lysine N-methyltransferase SETMAR | A histone-lysine N-methyltransferase SETMAR that is encoded in the genome of human. [PRO:DNx, UniProtKB:Q53H47] | Homo sapiens (human) |
Compounds (3)
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| (5-bromo-3-pyridinyl)-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone | aromatic carboxylic acid; pyridinemonocarboxylic acid | ||
| entecavir | benzamides; N-acylpiperidine | ||
| gsk343 | GSK343 : 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 |