Tclin EPAS1 Endothelial PAS domain-containing protein 1

Protein Summary

Description

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 APEX seems to activate CTAD (By similarity). This gene encodes a transcription factor involved in the induction of genes regulated by oxygen, which is induced as oxygen levels fall. The encoded protein contains a basic-helix-loop-helix domain protein dimerization domain as well as a domain found in proteins in signal transduction pathways which respond to oxygen levels. Mutations in this gene are associated with erythrocytosis familial type 4. [provided by RefSeq, Nov 2009]

Uniprot Accession IDs

• Q99814
• Q86VA2
• Q99630
• EPAS-1

Gene Name

• EPAS1

Ensembl ID

• ENST00000263734
• ENSP00000263734
• ENSG00000116016

Symbol

• BHLHE73
• HIF2A
• MOP2
• PASD2
• HLF
• MOP2
• ECYT4
• HIF2A
• PASD2
• bHLHe73

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
PubMedID	1
transcription factor perturbation	0.96
protein domain	0.92
biological process	0.91
gene perturbation	0.88

Protein Classes

PANTHER Classes

Protein / Transcription Factor / Basic Helix-loop-helix Transcription Factor / Endothelial Pas Domain-containing Protein 1

Protein / Nucleic Acid Binding / Endothelial Pas Domain-containing Protein 1

DTO Classes

Protein / Transcription Factor / Basic Helix-loop-helix Transcription Factor / Endothelial Pas Domain-containing Protein 1

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 391.43   (req: < 5)

Gene RIFs: 523   (req: <= 3)

Antibodies: 630   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 391.43   (req: >= 5)

Gene RIFs: 523   (req: > 3)

Antibodies: 630   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 30

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 83

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 1