OncoSignal
Live from Open Targets Platform, fetched 2026-11-11 16:09 UTC. Every row links to its source record.

KMT2E lysine methyltransferase 2E (inactive)

ENSG00000005483 · protein coding · Open Targets profile

Associates with chromatin regions downstream of transcriptional start sites of active genes and thus regulates gene transcription (PubMed:23629655, PubMed:23798402, PubMed:24130829). Chromatin interaction is mediated via the binding to tri-methylated histone H3 at 'Lys-4' (H3K4me3) (PubMed:23798402, PubMed:24130829). Key regulator of hematopoiesis involved in terminal myeloid differentiation and in the regulation of hematopoietic stem cell (HSCs) self-renewal by a mechanism that involves DNA methylation (By similarity). Also acts as an important cell cycle regulator, participating in cell cycle regulatory network machinery at multiple cell cycle stages including G1/S transition, S phase progression and mitotic entry (PubMed:14718661, PubMed:18573682, PubMed:19264965, PubMed:23629655). Recruited to E2F1 responsive promoters by HCFC1 where it stimulates tri-methylation of histone H3 at 'Lys-4' and transcriptional activation and thereby facilitates G1 to S phase transition (PubMed:23629655). During myoblast differentiation, required to suppress inappropriate expression of S-phase-promoting genes and maintain expression of determination genes in quiescent cells (By similarity). {ECO:0000250|UniProtKB:Q3UG20, ECO:0000269|PubMed:14718661, ECO:0000269|PubMed:18573682, ECO:0000269|PubMed:23629655, ECO:0000269|PubMed:23798402, ECO:0000269|PubMed:24130829}.

In 1 of 15 cancers, the evidence for KMT2E comes mainly from inherited variants

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.

Inherited (germline) variantsMutations in tumours (somatic)
00.250.50.751ovarian neoplasmovarian neoplasmovarian neoplasm: germline 0.24acute promyelocytic leukemiaacute promyelocytic leukemiaFamilial prostate cancerFamilial prostate cancerprostate cancerprostate cancerprostate carcinomaprostate carcinomaacute lymphoblastic leukemiaacute lymphoblastic leukemiaautoimmune lymphoproliferative syndromeautoimmune lymphoproliferative syndromeacute erythroblastic leukemiaacute erythroblastic leukemiaautoimmune lymphoproliferative syndrome…autoimmune lymphoproliferative syndrome due to CTLA4 haploinsufficiencyWiskott-Aldrich syndromeWiskott-Aldrich syndromeautoimmune lymphoproliferative syndrome…autoimmune lymphoproliferative syndrome type 4autoimmune lymphoproliferative syndrome…autoimmune lymphoproliferative syndrome type 1erythroleukemia, familial, susceptibili…erythroleukemia, familial, susceptibility tomyelodysplastic syndrome with ring side…myelodysplastic syndrome with ring sideroblastsX-linked lymphoproliferative syndromeX-linked lymphoproliferative syndrome

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

Antibody
UniProt loc high conf, GO CC med conf
PROTAC
UniProt Ubiquitination, Database Ubiquitination, Half-life Data

gnomAD loss of function constraint: o/e 0.16253000497817993 (upper bound 0.2204499989748001). 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 KMT2E's approved or late-stage drugs in the last three years.

No terminated, withdrawn or suspended trials of KMT2E'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.

DrugTypeHighest stageIndicationsSource records
No drugs or clinical candidates recorded.