Tclin EGFR Epidermal growth factor receptor

Protein Summary

Description

Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses (PubMed:2790960, PubMed:10805725, PubMed:27153536). Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF (PubMed:2790960, PubMed:7679104, PubMed:8144591, PubMed:9419975, PubMed:15611079, PubMed:12297049, PubMed:27153536, PubMed:20837704). Ligand binding triggers receptor homo- and/or heterodimerization and autophosphorylation on key cytoplasmic residues. The phosphorylated receptor recruits adapter proteins like GRB2 which in turn activates complex downstream signaling cascades. Activates at least 4 major downstream signaling cascades including the RAS-RAF-MEK-ERK, PI3 kinase-AKT, PLCgamma-PKC and STATs modules (PubMed:27153536). May also activate the NF-kappa-B signaling cascade (PubMed:11116146). Also directly phosphorylates other proteins like RGS16, activating its GTPase activity and probably coupling the EGF receptor signaling to the G protein-coupled receptor signaling (PubMed:11602604). Also phosphorylates MUC1 and increases its interaction with SRC and CTNNB1/beta-catenin (PubMed:11483589). Plays a role in enhancing learning and memory performance (By similarity). Isoform 2 may act as an antagonist of EGF action. (Microbial infection) Acts as a receptor for hepatitis C virus (HCV) in hepatocytes and facilitates its cell entry. Mediates HCV entry by promoting the formation of the CD81-CLDN1 receptor complexes that are essential for HCV entry and by enhancing membrane fusion of cells expressing HCV envelope glycoproteins. The protein encoded by this gene is a transmembrane glycoprotein that is a member of the protein kinase superfamily. This protein is a receptor for members of the epidermal growth factor family. EGFR is a cell surface protein that binds to epidermal growth factor. Binding of the protein to a ligand induces receptor dimerization and tyrosine autophosphorylation and leads to cell proliferation. Mutations in this gene are associated with lung cancer. [provided by RefSeq, Jun 2016]

Uniprot Accession IDs

• P00533
• O00688
• O00732
• P06268
• Q14225
• Q68GS5
• Q92795
• Q9BZS2
• Q9GZX1
• Q9H2C9
• Q9H3C9
• Q9UMD7
• Q9UMD8
• Q9UMG5

Gene Name

• EGFR

Ensembl ID

• ENST00000275493
• ENSP00000275493
• ENSG00000146648
• ENST00000342916
• ENSP00000342376
• ENST00000344576
• ENSP00000345973
• ENST00000420316
• ENSP00000413843

Symbol

• ERBB
• ERBB1
• HER1
• ERBB
• HER1
• mENA
• ERBB1
• PIG61
• NISBD2

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
biological term	1
chemical	1
hub protein	1
interacting protein	1

Protein Classes

DTO Classes

Protein / Kinase / Protein Kinase / Tk Group / Egfr Family / Epidermal Growth Factor Receptor

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: 19716.01   (req: < 5)

Gene RIFs: 5676   (req: <= 3)

Antibodies: 8544   (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: 19716.01   (req: >= 5)

Gene RIFs: 5676   (req: > 3)

Antibodies: 8544   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 115

Tchem

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

Active Ligands: 2419

Tclin

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

Active Drugs: 26