OncoSignal
Live from Open Targets Platform, fetched 2026-11-11 16:13 UTC. Every row links to its source record.

HIF1A hypoxia inducible factor 1 subunit alpha

ENSG00000100644 · protein coding · Open Targets profile

Functions as a master transcriptional regulator of the adaptive response to hypoxia (PubMed:11292861, PubMed:11566883, PubMed:15465032, PubMed:16973622, PubMed:17610843, PubMed:18658046, PubMed:20624928, PubMed:22009797, PubMed:30125331, PubMed:9887100). Under hypoxic conditions, activates the transcription of over 40 genes, including erythropoietin, glucose transporters, glycolytic enzymes, vascular endothelial growth factor, HILPDA, and other genes whose protein products increase oxygen delivery or facilitate metabolic adaptation to hypoxia (PubMed:11292861, PubMed:11566883, PubMed:15465032, PubMed:16973622, PubMed:17610843, PubMed:20624928, PubMed:22009797, PubMed:30125331, PubMed:9887100). Plays an essential role in embryonic vascularization, tumor angiogenesis and pathophysiology of ischemic disease (PubMed:22009797). Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Activation requires recruitment of transcriptional coactivators such as CREBBP and EP300 (PubMed:16543236, PubMed:9887100). Activity is enhanced by interaction with NCOA1 and/or NCOA2 (PubMed:10594042). Interaction with redox regulatory protein APEX1 seems to activate CTAD and potentiates activation by NCOA1 and CREBBP (PubMed:10202154, PubMed:10594042). Involved in the axonal distribution and transport of mitochondria in neurons during hypoxia (PubMed:19528298). {ECO:0000250|UniProtKB:Q61221, ECO:0000269|PubMed:10202154, ECO:0000269|PubMed:10594042, ECO:0000269|PubMed:11292861, ECO:0000269|PubMed:11566883, ECO:0000269|PubMed:15465032, ECO:0000269|PubMed:16543236, ECO:0000269|PubMed:16973622, ECO:0000269|PubMed:17610843, ECO:0000269|PubMed:18658046, ECO:0000269|PubMed:19528298, ECO:0000269|PubMed:20624928, ECO:0000269|PubMed:22009797, ECO:0000269|PubMed:30125331, ECO:0000269|PubMed:9887100}.

In 12 of 15 cancers, the evidence for HIF1A 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)
00.250.50.751Ollier diseaseOllier diseaseOllier disease: germline 0.62kidney neoplasmkidney neoplasmkidney neoplasm: somatic 0.61colorectal adenocarcinomacolorectal adenocarcinomacolorectal adenocarcinoma: somatic 0.61breast ductal adenocarcinomabreast ductal adenocarcinomabreast ductal adenocarcinoma: somatic 0.61brain glioblastomabrain glioblastomabrain glioblastoma: somatic 0.61lymphoid neoplasmlymphoid neoplasmlymphoid neoplasm: 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 0.61bile duct carcinomabile duct carcinomabile duct carcinoma: somatic 0.61ovarian endometrioid adenocarcinoma wit…ovarian endometrioid adenocarcinoma with squamous differentiationovarian endometrioid adenocarcinoma with squamous differentiation: somatic 0.61Maffucci syndromeMaffucci syndromeMaffucci syndrome: germline 0.60triple-negative breast carcinomatriple-negative breast carcinomatriple-negative breast carcinoma: germline 0.55breast carcinomabreast carcinomabreast carcinoma: somatic 0.46hepatocellular carcinomahepatocellular carcinomahepatocellular carcinoma: somatic 0.46non-small cell lung carcinomanon-small cell lung carcinomanon-small cell lung carcinoma: somatic 0.46

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, Druggable Family
PROTAC
UniProt Ubiquitination, Database Ubiquitination, Small Molecule Binder

gnomAD loss of function constraint: o/e 0.25891000032424927 (upper bound 0.36410999298095703). 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 HIF1A's approved or late-stage drugs in the last three years.

No terminated, withdrawn or suspended trials of HIF1A'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.