Protein / target
Endothelial PAS domain-containing protein 1
Protein at a glance
Biological role
Protein heterodimerization activity
Primary system
Cardiovascular system
Strongest disease association
erythrocytosis, familial, 4
Therapeutic maturity
Clinically validated target
Druggability
Small molecule
Clinical development
1 approved
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function
Transcription factor involved in the induction of oxygen regulated genes. Heterodimerizes with ARNT; heterodimer binds to core DNA sequence 5'-TACGTG-3' within the hypoxia response element (HRE) of target gene promoters (By similarity). Regulates the vascular endothelial growth factor (VEGF) expression and seems to be implicated in the development of blood vessels and the tubular system of lung. May also play a role in the formation of the endothelium that gives rise to the blood brain barrier. Potent activator of the Tie-2 tyrosine kinase expression. Activation requires recruitment of transcriptional coactivators such as CREBBP and probably EP300. Interaction with redox regulatory protein APEX1 seems to activate CTAD (By similarity)
Subcellular location
Domains and Gene Ontology detail (31)Hide
Domains & features
Gene Ontology
- Cchromatin
- Ccytosol
- Cnuclear speck
- Cnucleoplasm
- Cnucleus
- Ctranscription regulator complex
- FDNA-binding transcription activator activity, RNA polymerase II-specific
- FDNA-binding transcription factor activity, RNA polymerase II-specific
- Fprotein heterodimerization activity
- FRNA polymerase II cis-regulatory region sequence-specific DNA binding
- FRNA polymerase II transcription regulatory region sequence-specific DNA binding
- FRNA polymerase II-specific DNA-binding transcription factor binding
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
View supporting evidenceHide supporting evidence
Transcriptional regulation
- ·Transcription factor involved in the induction of oxygen regulated genes. Heterodimerize…
- ·transcription regulator complex
- ·DNA-binding transcription activator activity, RNA polymerase II-specific
- ·DNA-binding transcription factor activity, RNA polymerase II-specific
Nuclear receptor signalling
- ·DNA-binding transcription factor activity, RNA polymerase II-specific
View underlying pathways (8)Hide underlying pathways
Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.
Interaction neighbourhood
Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.
Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.
Drugs targeting this protein
Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.
Endothelial PAS domain-containing protein 1 inhibitor
Appears in clinical studies involving von Hippel-Lindau disease, renal cell carcinoma, neoplasm, hemangioblastoma
ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.
Translational evidence
Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.
Strongest genetic associations
Human genetic evidence — the most direct causal link between this target and a disease.
Highest-confidence therapeutic associations
Diseases where a drug acting on this target has already reached clinical development.
Show all associationsHide all associations
Open Targets ranks 1,273 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.
Known drugs · 1 total
von Hippel-Lindau disease · renal cell carcinoma · neoplasm
Tractability
Safety liabilities
Clinical trials
Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.
Show remaining trials (24)Hide
ClinicalTrials.gov via the drug-target graph.
Forefront confidence
Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.
The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.
What's happening now
Recent activity around this target, drawn from one canonical event stream. Every item is reached through a drug that targets this protein, so each event is news about that drug rather than about the protein directly.
- Regulatory actionMerck's Welireg-Keytruda pairing sticks the landing in adjuvant kidney cancer treatment with new FDA nod
- Indication expanded
Indication expansion: BELZUTIFAN (NDA215383)
- Indication expanded
Indication expansion: BELZUTIFAN (NDA215383)
- Indication expanded
Indication expansion: BELZUTIFAN (NDA215383)
- Indication expanded
Indication expansion: BELZUTIFAN (NDA215383)
- Regulatory approval
Approval: Welireg (EMA)
- Label change
Label change: BELZUTIFAN (NDA215383)
- Indication expanded
Indication expansion: BELZUTIFAN (NDA215383)
- New publicationBelzutifan for Renal Cell Carcinoma in von Hippel-Lindau Disease.
- Regulatory approval
Approval: BELZUTIFAN (NDA215383)
Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.