Topoisomerase II alpha (TOP2A)
The enzyme that cuts both DNA strands to untangle chromosomes before cell division. Etoposide and the anthracyclines hold it in the cut state, filling dividing cells with double-strand breaks.
Overview
Topoisomerase II alpha passes one DNA double helix through a transient break in another, decatenating replicated chromosomes and relaxing supercoils; its expression peaks in proliferating cells. Etoposide and anthracyclines such as doxorubicin stabilise the covalent enzyme-DNA complex, converting a normal catalytic step into lasting double-strand breaks. Etoposide is central to small-cell lung cancer, germ cell tumour and lymphoma regimens; anthracyclines to breast cancer, lymphoma and sarcoma regimens. Therapy-related leukaemia with KMT2A rearrangement and anthracycline cardiotoxicity are the class hazards.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · The enzyme that cuts both DNA strands to untangle chromosomes before cell division. Etoposide and the anthracyclines hold it in the cut state, filling dividing cells with double-strand breaks.
- 1 · What it is
The enzyme that cuts both DNA strands to untangle chromosomes before cell division. Etoposide and the anthracyclines hold it in the cut state, filling dividing cells with double-strand breaks.
- 2 · What goes wrong in cancer
Type IIA topoisomerase, proliferation-associated isoform; poisoned by etoposide and anthracyclines into a stable cleavage complex.
- 3 · How drugs use it
No product in this corpus aims at Topoisomerase II alpha (TOP2A) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Biology
Type IIA topoisomerase, proliferation-associated isoform; poisoned by etoposide and anthracyclines into a stable cleavage complex.
- Proliferating tumour cells; TOP2A amplification in a subset of HER2-positive breast cancers
Latest papers
topQuery for this target: (TITLE:"Topoisomerase II alpha" OR ABSTRACT:"Topoisomerase II alpha" OR TITLE:"TOP2A" OR ABSTRACT:"TOP2A") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Topoisomerase II alpha (TOP2A), not a curated reading list.
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