Topoisomerase inhibitor

Topoisomerase inhibitors are chemotherapy agents designed to interfere with the action of topoisomerase enzymes (topoisomerase I and II), which are enzymes that control the changes in DNA structure by catalyzing the breaking and rejoining of the phosphodiester backbone of DNA strands during the normal cell cycle.

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In recent years, topoisomerase inhibitors have become popular targets for cancer chemotherapy treatments. It is thought that topoisomerase inhibitors block the ligation step of the cell cycle, and that topoisomerase I and II inhibitors interfere with the transcription and replication of DNA by upsetting proper DNA supercoiling.

A commonly prescribed class of topoisomerase inhibitors are fluoroquinolones.

• Topoisomerase I inhibitors: irinotecan, topotecan, camptothecin and lamellarin D
• Topoisomerase II inhibitors: amsacrine, etoposide, etoposide phosphate, teniposide and doxorubicin