Protein / target
Epidermal growth factor receptor
Protein at a glance
Biological role
Transmembrane receptor protein tyrosine kinase
Primary biology
EGFR/ERBB growth-factor signalling
Strongest disease association
Squamous Cell Carcinoma of Head and Neck
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
Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses.
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Receptor tyrosine kinase binding ligands of the EGF family and activating several signaling cascades to convert extracellular cues into appropriate cellular responses (PubMed:10805725, PubMed:27153536, PubMed:2790960, PubMed:35538033). Known ligands include EGF, TGFA/TGF-alpha, AREG, epigen/EPGN, BTC/betacellulin, epiregulin/EREG and HBEGF/heparin-binding EGF (PubMed:12297049, PubMed:15611079, PubMed:17909029, PubMed:20837704, PubMed:27153536, PubMed:2790960, PubMed:7679104, PubMed:8144591, PubMed:9419975). 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). Positively regulates cell migration via interaction with CCDC88A/GIV which retains EGFR at the cell membrane following ligand stimulation, promoting EGFR signaling which triggers cell migration (PubMed:20462955). Plays a role in enhancing learning and memory performance (By similarity). Plays a role in mammalian pain signaling (long-lasting hypersensitivity) (By similarity)
Subcellular location
Domains and Gene Ontology detail (84)Hide
Domains & features
Gene Ontology
- Cbasal plasma membrane
- Cbasolateral plasma membrane
- Ccell junction
- Ccell surface
- Cclathrin-coated endocytic vesicle membrane
- Ccytoplasm
- Cearly endosome membrane
- Cendoplasmic reticulum membrane
- Cendosome
- Cendosome membrane
- Cextracellular space
- Cfocal adhesion
Biological roles
What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.
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Receptor tyrosine kinase signalling
- ·Receptor tyrosine kinase binding ligands of the EGF family and activating several signal…
- ·transmembrane receptor protein tyrosine kinase activity
- ·ERBB2-EGFR signaling pathway
- ·Signaling by ERBB2
Cell migration
- ·Receptor tyrosine kinase binding ligands of the EGF family and activating several signal…
- ·positive regulation of cell migration
- ·ERBB2 Regulates Cell Motility
Growth-factor signalling
- ·epidermal growth factor binding
- ·epidermal growth factor receptor activity
- ·cellular response to epidermal growth factor stimulus
- ·epidermal growth factor receptor signaling pathway
Cell proliferation & survival
- ·positive regulation of cell population proliferation
- ·PIP3 activates AKT signaling
- ·PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling
Oncogenic signalling
- ·Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
- ·Constitutive Signaling by Aberrant PI3K in Cancer
Cell-cycle regulation
- ·positive regulation of G1/S transition of mitotic cell cycle
View underlying pathways (25)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.
28 medicines meet Open Targets' target-level approved-medicine definition; the 6 shown here are those on this page with a canonical approved disease indication in the graph. 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.
Epidermal growth factor receptor erbB1 inhibitor
Indicated for Carcinoma, Non-Small-Cell Lung, Neoplasms
Epidermal growth factor receptor erbB1 inhibitor
Indicated for Neoplasms
Epidermal growth factor receptor erbB1 inhibitor
Indicated for Carcinoma, Non-Small-Cell Lung, Neoplasms
Epidermal growth factor receptor erbB1 inhibitor
Epidermal growth factor receptor erbB1 inhibitor
Indicated for Carcinoma, Non-Small-Cell Lung, Pancreatic Neoplasms
Epidermal growth factor receptor erbB1 inhibitor
View all 10 targeting drugsHide
Epidermal growth factor receptor erbB1 inhibitor
Indicated for Neoplasms
Epidermal growth factor receptor erbB1 inhibitor
Epidermal growth factor receptor erbB1 inhibitor
Indicated for Carcinoma, Non-Small-Cell Lung, Neoplasms
Epidermal growth factor receptor erbB1 inhibitor
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 EGFR
Gene-level evidence surfaced through the gene EGFRthat 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
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
82 compounds recorded · 28 approved · 53 in clinical development · 1 earlier-stage
View all recorded compounds (10)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
Antibodies — Strong
Protein degraders — Emerging
Other modalities — Strong
View underlying tractability evidence (17)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 9 drugs that target 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.
- Trial status changed
Phase I Study of the Pan-ERBB Inhibitor Neratinib Given in Combination With Everolimus, Palbociclib, or Trametinib in Advanced Cancer Subjects With EGFR Mutation/Amplification, HER2 Mutation/Amplification, or HER3/4 Mutation or KRAS Mutation
- Regulatory approval
Approval: Lazcluze (EMA)
- Withdrawn from market
Market withdrawal: Gefitinib Mylan (EMA)
- New publicationAmivantamab plus Lazertinib in Previously Untreated <i>EGFR</i>-Mutated Advanced NSCLC.
- New publicationPyrotinib versus placebo in combination with trastuzumab and docetaxel as first line treatment in patients with HER2 positive metastatic breast cancer (PHILA): randomised, double blind, multicentre, phase 3 trial.
- New publicationNimotuzumab Plus Gemcitabine for K-Ras Wild-Type Locally Advanced or Metastatic Pancreatic Cancer.
- New publicationCurrent treatment strategies for EGFR-mutated non-small cell lung cancer: from first line to beyond osimertinib resistance.
- New publicationAdjuvant Osimertinib for Resected EGFR-Mutated Stage IB-IIIA Non-Small-Cell Lung Cancer: Updated Results From the Phase III Randomized ADAURA Trial.
- New publicationTherapeutic strategies for EGFR-mutated non-small cell lung cancer patients with osimertinib resistance.
- New publicationTreatment Outcomes and Safety of Mobocertinib in Platinum-Pretreated Patients With EGFR Exon 20 Insertion-Positive Metastatic Non-Small Cell Lung Cancer: A Phase 1/2 Open-label Nonrandomized Clinical Trial.
- Regulatory approval
Approval: Rybrevant (EMA)
- Regulatory approval
Approval: Alunbrig (EMA)
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.
Related family literature
Papers about “ErbB Receptors” — a broader family this protein belongs to. Shown as context; not counted as papers specifically about this protein.
via ErbB Receptors
via ErbB Receptors
via ErbB Receptors
via ErbB Receptors
via ErbB Receptors
via ErbB Receptors
via ErbB Receptors
Europe PMC literature, reached through curated HGNC family membership. Membership is a taxonomic relationship — it does not imply this protein participates in every mechanism these papers discuss.