DNA methyltransferase 3A (DNMT3A)
DNMT3A writes new methyl marks on DNA; it is one of the most commonly mutated genes in acute myeloid leukaemia and is trapped by the hypomethylating drugs azacitidine and decitabine.
Overview
DNA methyltransferase 3A establishes new (de novo) cytosine methylation. Loss-of-function mutations, most often at R882, are among the commonest events in acute myeloid leukaemia and in age-related clonal haematopoiesis. Azacitidine and decitabine are incorporated into DNA and covalently trap DNA methyltransferases, including DNMT3A, leading to their degradation and to demethylation.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · DNMT3A writes new methyl marks on DNA; it is one of the most commonly mutated genes in acute myeloid leukaemia and is trapped by the hypomethylating drugs azacitidine and decitabine.
- 1 · What it is
DNMT3A writes new methyl marks on DNA; it is one of the most commonly mutated genes in acute myeloid leukaemia and is trapped by the hypomethylating drugs azacitidine and decitabine.
- 2 · What goes wrong in cancer
A de novo methyltransferase working with DNMT3L during development and in haematopoietic stem cells; the R882H mutant acts dominantly to reduce methylation.
- 3 · How drugs use it
No product in this corpus aims at DNA methyltransferase 3A (DNMT3A) yet. Inhibitors are shaped to fit the enzyme's active site so the reaction the cancer relies on stops.
External identifiers
Biology
A de novo methyltransferase working with DNMT3L during development and in haematopoietic stem cells; the R882H mutant acts dominantly to reduce methylation.
- Haematopoietic stem cells
- Mutated in a large share of AML and in clonal haematopoiesis
How often this target appears
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Acute myeloid leukaemia | 22.1% | DNMT3A mutation, exon sequencing of 281 de novo AML cases (62 mutated) | 33.7% in intermediate-risk cytogenetics and absent in favourable-risk disease; R882 the commonest site | doi.org |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
Latest papers
topQuery for this target: (TITLE:"DNA methyltransferase 3A" OR ABSTRACT:"DNA methyltransferase 3A" OR TITLE:"DNMT3A" OR ABSTRACT:"DNMT3A") 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 DNA methyltransferase 3A (DNMT3A), not a curated reading list.
Similar pages
not linked directly; found by shared links- CompanyOrca Biosystems
Shares Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.
- CompanyOtsuka Pharmaceutical
Shares Decitabine, Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.
- CompanyTreadwell Therapeutics
Shares Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.
- CompanyAptose Biosciences
Shares Azacitidine, Acute myeloid leukaemia.
- PersonMarc H.G.P. Raaijmakers
Shares Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.
- PersonUwe Platzbecker
Shares Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.
- InstitutionUSC Norris Comprehensive Cancer Center
Shares Azacitidine, Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.
- TermHypomethylating agents (azacitidine, decitabine)
Shares Azacitidine, Myelodysplastic syndromes / neoplasms (MDS), Acute myeloid leukaemia.