Protein / target
Endothelial PAS domain-containing protein 1
Protein at a glance
Biological role
Protein heterodimerization
Strongest disease association
Erythrocytosis, familial, 4
Therapeutic position
Established drug target
Derived from structured UniProt, Open Targets and literature data on this page.
Protein profile
Canonical identity and biological annotation from UniProt.
Function overview
Transcription factor involved in the induction of oxygen regulated genes.
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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.
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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
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.
Approved medicines with mapped indications
Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.
Broader indication categories (1)Hide
Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.
Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.
Drugs targeting this protein
How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.
Endothelial PAS domain-containing protein 1 inhibitor
Indicated for Carcinoma, Renal Cell, Hemangioblastoma, Neuroendocrine Tumors, von Hippel-Lindau Disease
ChEMBL mechanism, action type, target identity and approved indications. Open Targets clinical status.
Translational evidence
Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.
Strongest disease associations · via encoding gene EPAS1
Gene-level evidence surfaced through the gene EPAS1that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.
View evidence synthesis (5)Hide
This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. 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 per-type scores above show the calculation.
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Drug development
1 compounds recorded · 1 approved
View all recorded compounds (1)Hide
Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.
Tractability
Small molecules — Strong
Protein degraders — Emerging
View underlying tractability evidence (8)Hide
Raw Open Targets tractability assessment buckets, by modality.
Safety-related annotations
Terms indexed against this target in Open Targets' safety data, with their datasource. These are annotations, not causal claims: the direction of effect (whether activation or inhibition is implicated), species and evidence strength are not captured here, so an entry does not mean that modulating this target is known to cause that condition.
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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.
View all trials (26)Hide
ClinicalTrials.gov via the drug-target graph.
What's happening now
Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for a drug that targets this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.
- 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.