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Irinotecan topoisomerase I complex
- Molecular classification
- Enzyme-DNA complex, Drug-Target Complex
01
Overview
The irinotecan topoisomerase I complex refers to the ternary molecular assembly formed when irinotecan (or its active metabolite SN-38) binds to DNA topoisomerase I covalently linked to DNA. This interaction is central to irinotecan's cytotoxic mechanism. Irinotecan/SN-38 stabilizes the covalent complex, preventing religation of DNA breaks induced by topoisomerase I. This leads to double-strand DNA breaks upon collision with the replication machinery, resulting in cell death.
- Other names
- SN-38 topoisomerase I complexTopoI-DNA-Irinotecan complexTopoI-DNA-SN-38 complex
02
Mechanism of action
Stabilization of TopoI-DNA cleavage complexes; prevents religation; ultimately leading to double-strand breaks upon replication fork collision.
03
Biological functions
DNA replication interferenceDNA transcription interferenceApoptosis inductionCell cycle arrest
04
Disease associations
Cancer
05
Safety considerations
MyelosuppressionDiarrheaNeutropeniaDrug resistance
06
Interacting drugs
Irinotecan
1 more in the full profile.
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