OncoSignal
Live from Open Targets Platform, fetched 2026-11-12 04:47 UTC. Every row links to its source record.

KDM6A lysine demethylase 6A

ENSG00000147050 · protein coding · Open Targets profile

Histone demethylase that specifically demethylates 'Lys-27' of histone H3, thereby playing a central role in histone code (PubMed:17713478, PubMed:17761849, PubMed:17851529). Demethylates trimethylated and dimethylated but not monomethylated H3 'Lys-27' (PubMed:17713478, PubMed:17761849, PubMed:17851529). Plays a central role in regulation of posterior development, by regulating HOX gene expression (PubMed:17851529). Demethylation of 'Lys-27' of histone H3 is concomitant with methylation of 'Lys-4' of histone H3, and regulates the recruitment of the PRC1 complex and monoubiquitination of histone H2A (PubMed:17761849). Plays a demethylase-independent role in chromatin remodeling to regulate T-box family member-dependent gene expression (By similarity). {ECO:0000250|UniProtKB:O70546, ECO:0000269|PubMed:17713478, ECO:0000269|PubMed:17761849, ECO:0000269|PubMed:17851529, ECO:0000269|PubMed:18003914}.

In 15 of 15 cancers, the evidence for KDM6A comes mainly from mutations found in tumours

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)
00.250.50.751urinary bladder cancerurinary bladder cancerurinary bladder cancer: somatic 0.91urinary bladder carcinomaurinary bladder carcinomaurinary bladder carcinoma: somatic 0.80prostate adenocarcinomaprostate adenocarcinomaprostate adenocarcinoma: somatic 0.76squamous cell lung carcinomasquamous cell lung carcinomasquamous cell lung carcinoma: somatic 0.63bladder transitional cell carcinomabladder transitional cell carcinomabladder transitional cell carcinoma: somatic 0.61urothelial carcinomaurothelial carcinomaurothelial carcinoma: somatic 0.61lung carcinomalung carcinomalung carcinoma: somatic 0.61breast ductal adenocarcinomabreast ductal adenocarcinomabreast ductal adenocarcinoma: somatic 0.61exocrine pancreatic carcinomaexocrine pancreatic carcinomaexocrine pancreatic carcinoma: somatic 0.61lymphoid neoplasmlymphoid neoplasmlymphoid neoplasm: somatic 0.61bile duct carcinomabile duct carcinomabile duct carcinoma: somatic 0.61Meningothelial MeningiomaMeningothelial MeningiomaMeningothelial Meningioma: somatic 0.61carcinoma of liver and intrahepatic bil…carcinoma of liver and intrahepatic biliary tractcarcinoma of liver and intrahepatic biliary tract: somatic 0.61endometrial endometrioid adenocarcinomaendometrial endometrioid adenocarcinomaendometrial endometrioid adenocarcinoma: somatic 0.61Angiomatous MeningiomaAngiomatous MeningiomaAngiomatous Meningioma: somatic 0.61

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, Med-Quality Pocket
PROTAC
Database Ubiquitination, Half-life Data, Small Molecule Binder

gnomAD loss of function constraint: o/e 0.09357199817895889 (upper bound 0.15488000214099884). 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 KDM6A's approved or late-stage drugs in the last three years.

No terminated, withdrawn or suspended trials of KDM6A'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.