DOT1L DOT1 like histone lysine methyltransferase
ENSG00000104885 · protein coding · Open Targets profile
Histone methyltransferase that methylates 'Lys-79' of histone H3 (PubMed:12123582, PubMed:38503750, PubMed:38129415). Histones in nucleosomes are preferred as substrate compared to free histones (PubMed:12123582, PubMed:38503750). Binds to DNA (PubMed:12628190, PubMed:38503750). Together with MLLT3/AF9, is involved in SCNN1A transcriptional repression following H3K79 hypermethylation at the promoter (By similarity). {ECO:0000250|UniProtKB:Q6XZL8, ECO:0000269|PubMed:12123582, ECO:0000269|PubMed:12628190, ECO:0000269|PubMed:38129415, ECO:0000269|PubMed:38503750}.
Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.
Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.
Tractability
- Small molecule
- Structure with Ligand, High-Quality Ligand, High-Quality Pocket, Druggable Family
- PROTAC
- Database Ubiquitination, Small Molecule Binder
gnomAD loss of function constraint: o/e 0.21528999507427216 (upper bound 0.28786998987197876). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.
Who runs trials of these drugs
No named investigators on registry trials of DOT1L's approved or late-stage drugs in the last three years.
No terminated, withdrawn or suspended trials of DOT1L's drugs are registered
All 0 drugs and clinical candidates as a table
Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.
| Drug | Type | Highest stage | Indications | Source records |
|---|---|---|---|---|
| No drugs or clinical candidates recorded. | ||||