Which chemotherapy drugs are topoisomerase inhibitors?
Topoisomerase I inhibitors include irinotecan, topotecan, and camptothecin, and topoisomerase II inhibitors include etoposide, doxorubicin, and epirubicin.
What are topoisomerase 1 inhibitors?
Topoisomerase I inhibitors are a new class of anticancer agents with a mechanism of action aimed at interrupting DNA replication in cancer cells, the result of which is cell death. Most if not all Topoisomerase I inhibitors are derivatives of the plant extract camptothecin.
What are topoisomerase 2 inhibitors?
Topoisomerase II is an enzyme essential for DNA replication, chromosome condensation and chromosome segregation. Inhibitors of topoisomerase II are important drugs used in the therapy of many neoplasms including breast cancer, lung cancer, testicular cancer, lymphomas and sarcomas.
Is etoposide topoisomerase inhibitor?
Etoposide was the first agent recognised as a topoisomerase II inhibiting anticancer drug. Research on etoposide has helped the understanding of mechanisms by which drugs poison topoisomerase II.
Which of the following drugs inhibits bacterial topoisomerase?
Fluoroquinolones. Fluoroquinolones inhibit bacterial cell proliferation by inhibiting DNA gyrase and topoisomerase IV, both essential enzymes in bacterial DNA transcription and replication (Hooper, 2001).
Is irinotecan a topoisomerase inhibitor?
UGT1A and Irinotecan Irinotecan is a topoisomerase I inhibitor used to treat several solid tumor types, including CRC, in combination with other chemotherapeutic agents.
How do topoisomerase II inhibitors work?
Inhibitors of the mammalian enzymes are widely used antitumor drugs. They stabilize topoisomerase-DNA cleavable complexes by hindering the DNA relegating step of the catalytic reaction, thus resulting in DNA cleavage stimulation. Topoisomerase II inhibitors may also have genotoxic effects.
Which drugs inhibit topoisomerase enzymes?
Drugs in the Subclass Topoisomerase Inhibitors:
- Etoposide.
- Irinotecan.
- Teniposide.
- Topotecan.
How does doxorubicin inhibit topoisomerase?
Doxorubicin inhibits topoisomerase II, which overwinds DNA during transcription, thereby preventing the recombination of the DNA double strand, thus stopping DNA replication2.
Does bleomycin inhibit topoisomerase?
Antitumor antibiotics or topoisomerase inhibitors include doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxantrone, and bleomycin.
How does etoposide inhibit topoisomerase?
Etoposide kills cells by stabilizing a covalent enzyme-cleaved DNA complex (known as the cleavage complex) that is a transient intermediate in the catalytic cycle of topoisomerase II. If these breaks overwhelm the cell, they can initiate death pathways.
Are anthracyclines topoisomerase inhibitors?
Anthracyclines are a class of potent and widely used cytotoxic drugs, derived from antibiotics that inhibit DNA and RNA synthesis by intercalating between base pairs of the DNA/RNA strand. They create iron-mediated free oxygen radicals, damaging the DNA and cell membranes, and inhibit topoisomerase II.