Target intelligence / Profile preview

Topoisomerase Inhibition (Topo Inhibition)

Target
Topo Inhibition
Molecular classification
Enzyme Inhibition
01

Overview

Topoisomerase inhibition refers to the process of blocking the activity of topoisomerases, which are essential enzymes that regulate DNA topology during critical cellular processes such as replication, transcription, and recombination. There are two main types of topoisomerases targeted by inhibitors: Topoisomerase I (Top1) and Topoisomerase II (Top2). Inhibitors block the action of topoisomerases, leading to accumulation of DNA damage. This results in persistent DNA breaks that can trigger cell cycle arrest or apoptosis. Many topoisomerase inhibitors are used as chemotherapeutic agents due to their ability to induce lethal DNA damage selectively in rapidly dividing tumor cells.

Other names
Topoisomerase I InhibitionTopoisomerase II InhibitionDNA Topoisomerase Inhibition
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Mechanism of action

Inhibitors block the action of topoisomerases, leading to accumulation of DNA damage by stabilizing the enzyme-DNA cleavage complex at single-stranded or double-stranded nicks, preventing re-ligation or strand passage. This results in persistent DNA breaks that can trigger cell cycle arrest or apoptosis.

03

Biological functions

Cell proliferationDNA replicationDNA transcriptionDNA recombinationCell cycle arrestApoptosis
04

Disease associations

CancerInfection
05

Safety considerations

FatigueGastrointestinal disturbances (diarrhea)Hair lossAnemiaIncreased infection riskCardiac toxicitySecondary malignanciesGenotoxic effects on non-cancerous cellsSecondary leukemias
06

Interacting drugs

Camptothecin

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