DNMT1 (DNA methyltransferase 1)
The enzyme that copies methylation marks onto newly made DNA, keeping genes silenced. Azacitidine and decitabine trap and destroy it, waking silenced tumour suppressor genes in blood cancers.
Overview
DNMT1 maintains DNA methylation by copying the pattern from the parent strand to the new strand after replication. Azacitidine and decitabine are cytidine analogues incorporated into DNA that covalently trap DNMT1, which is then degraded, so methylation is lost over successive cell divisions and silenced genes are re-expressed; at higher doses they are also directly cytotoxic. They are standard treatment for higher-risk myelodysplastic syndromes and, with venetoclax, for older or unfit patients with acute myeloid leukaemia. Oral decitabine with cedazuridine matches intravenous exposure.
- 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 copies methylation marks onto newly made DNA, keeping genes silenced. Azacitidine and decitabine trap and destroy it, waking silenced tumour suppressor genes in blood cancers.
- 1 · What it is
The enzyme that copies methylation marks onto newly made DNA, keeping genes silenced. Azacitidine and decitabine trap and destroy it, waking silenced tumour suppressor genes in blood cancers.
- 2 · What goes wrong in cancer
Maintenance DNA methyltransferase acting at hemimethylated CpG sites after replication; covalently trapped by incorporated azacytosine.
- 3 · How drugs use it
No product in this corpus aims at DNMT1 (DNA methyltransferase 1) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Biology
Maintenance DNA methyltransferase acting at hemimethylated CpG sites after replication; covalently trapped by incorporated azacytosine.
- Myelodysplastic syndromes
- Acute myeloid leukaemia
- Chronic myelomonocytic leukaemia
Latest papers
topQuery for this target: (TITLE:"DNMT1" OR ABSTRACT:"DNMT1" OR TITLE:"DNA methyltransferase 1" OR ABSTRACT:"DNA methyltransferase 1") 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 DNMT1 (DNA methyltransferase 1), not a curated reading list.
Similar pages
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