Target Information
| Target General Information | Top | |||||
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| Target ID |
T79157
(Former ID: TTDI02062)
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| Target Name |
Epiregulin (EREG)
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| Synonyms |
l=Epiregulin; Proepiregulin; EPR
Click to Show/Hide
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| Gene Name |
EREG
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Chronic kidney disease [ICD-11: GB61] | |||||
| Function |
Stimulates EGFR and ERBB4 tyrosine phosphorylation. Contributes to inflammation, wound healing, tissue repair, and oocyte maturation by regulating angiogenesis and vascular remodeling and by stimulating cell proliferation. Ligand of the EGF receptor/EGFR and ERBB4.
Click to Show/Hide
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| BioChemical Class |
Growth factor
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| UniProt ID | ||||||
| Sequence |
MTAGRRMEMLCAGRVPALLLCLGFHLLQAVLSTTVIPSCIPGESSDNCTALVQTEDNPRV
AQVSITKCSSDMNGYCLHGQCIYLVDMSQNYCRCEVGYTGVRCEHFFLTVHQPLSKEYVA LTVILIILFLITVVGSTYYFCRWYRNRKSKEPKKEYERVTSGDPELPQV Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | LY3016859 | Drug Info | Phase 1/2 | Chronic kidney disease | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | LY3016859 | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Pathway Affiliation
of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.
Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes
(Pharmacol Rev, 58: 259-279, 2006).
Biological Network Descriptors
of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.
The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information
(Front Pharmacol, 9, 1245, 2018;
Curr Opin Struct Biol. 44:134-142, 2017).
Human Similarity Proteins
Human Pathway Affiliation
Biological Network Descriptors
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| KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
|---|---|---|---|
| MAPK signaling pathway | hsa04010 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| ErbB signaling pathway | hsa04012 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| PI3K-Akt signaling pathway | hsa04151 | Affiliated Target |
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| Class: Environmental Information Processing => Signal transduction | Pathway Hierarchy | ||
| Degree | 7 | Degree centrality | 7.52E-04 | Betweenness centrality | 1.16E-05 |
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| Closeness centrality | 2.27E-01 | Radiality | 1.40E+01 | Clustering coefficient | 7.62E-01 |
| Neighborhood connectivity | 6.20E+01 | Topological coefficient | 2.49E-01 | Eccentricity | 12 |
| Download | Click to Download the Full PPI Network of This Target | ||||
| Target Regulators | Top | |||||
|---|---|---|---|---|---|---|
| Target-regulating microRNAs | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| KEGG Pathway | [+] 1 KEGG Pathways | + | ||||
| 1 | ErbB signaling pathway | |||||
| NetPath Pathway | [+] 2 NetPath Pathways | + | ||||
| 1 | FSH Signaling Pathway | |||||
| 2 | EGFR1 Signaling Pathway | |||||
| Panther Pathway | [+] 1 Panther Pathways | + | ||||
| 1 | EGF receptor signaling pathway | |||||
| PID Pathway | [+] 2 PID Pathways | + | ||||
| 1 | ErbB4 signaling events | |||||
| 2 | ErbB receptor signaling network | |||||
| Reactome | [+] 9 Reactome Pathways | + | ||||
| 1 | SHC1 events in ERBB2 signaling | |||||
| 2 | PI3K events in ERBB4 signaling | |||||
| 3 | SHC1 events in ERBB4 signaling | |||||
| 4 | Nuclear signaling by ERBB4 | |||||
| 5 | PIP3 activates AKT signaling | |||||
| 6 | GRB2 events in ERBB2 signaling | |||||
| 7 | PI3K events in ERBB2 signaling | |||||
| 8 | Constitutive Signaling by Aberrant PI3K in Cancer | |||||
| 9 | RAF/MAP kinase cascade | |||||
| WikiPathways | [+] 4 WikiPathways | + | ||||
| 1 | ErbB Signaling Pathway | |||||
| 2 | Signaling by ERBB4 | |||||
| 3 | Signaling by ERBB2 | |||||
| 4 | PIP3 activates AKT signaling | |||||
| References | Top | |||||
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| REF 1 | Generation and activity of a humanized monoclonal antibody that selectively neutralizes the epidermal growth factor receptor ligands transforming growth factor-alpha and epiregulin. J Pharmacol Exp Ther. 2014 May;349(2):330-43. | |||||
| REF 2 | ClinicalTrials.gov (NCT01774981) Study of LY3016859 in Participants With Diabetic Nephropathy. U.S. National Institutes of Health. | |||||
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