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Epidermal growth factor receptor (EGFR), Erb-B2 receptor tyrosine kinase (ErbB2), and Erb-B4 receptor tyrosine kinase (ErbB4) (EGFR (for Epidermal growth factor receptor), ErbB2 (for Erb-B2 receptor tyrosine kinase), ErbB4 (for Erb-B4 receptor tyrosine kinase))

Target
EGFR (for Epidermal growth factor receptor), ErbB2 (for Erb-B2 receptor tyrosine kinase), ErbB4 (for Erb-B4 receptor tyrosine kinase)
Molecular classification
Receptor tyrosine kinase (RTK), Membrane receptor, Cell surface receptor, Enzyme (kinase activity), Signal transducer
01

Overview

The ErbB receptor family consists of four structurally related receptor tyrosine kinases: Epidermal growth factor receptor (EGFR, also known as ErbB1/HER1), Erb-B2 receptor tyrosine kinase (ErbB2/HER2/Neu), Erb-B3 receptor tyrosine kinase (ErbB3/HER3), and Erb-B4 receptor tyrosine kinase (ErbB4/HER4). These receptors possess an extracellular ligand-binding domain, a transmembrane domain, and an intracellular tyrosine kinase domain. They mediate cellular responses after ligand binding and dimerization, resulting in autophosphorylation and recruitment of intracellular signaling proteins. EGFR and ErbB2 are critical drivers in several cancers; targeted therapies against them are among the most successful examples of precision oncology. ErbB4 is less studied but plays important roles in neural development and is also implicated in some cancers. When activated abnormally, these receptors contribute to oncogenesis, tumor progression, and therapy resistance[1][2][3][5][7][9]. EGFR/ErbB2/ErbB4 are collectively key drug targets—yet each functions distinctly; in clinical and research contexts, they are usually considered separately for therapeutic decision-making. The use of the combined "EGFR/ErbB2/ErbB4" nomenclature is inaccurate for structured data or mechanistic studies, so the grouping is best split into its respective members for detailed annotation[1][5][9].

Other names
ErbB1HER1HER2NeuHER4ErbB receptor familyEGFR familysubclass I RTK superfamily
02

Mechanism of action

Small molecule kinase inhibitors (inhibit ATP binding in tyrosine kinase domain) Monoclonal antibodies (block ligand binding or receptor dimerization) Antibody-drug conjugates (targeted delivery of cytotoxic agents) Downregulation, degradation of receptor, blockade of downstream signaling

03

Biological functions

Signal transductionCell proliferationCell differentiationCell survival and apoptosisCell migrationAngiogenesis
04

Disease associations

Cancer (especially non-small cell lung cancer, breast cancer, glioma, ovarian, gastric, bladder)Other (roles in developmental abnormalities by abnormal signaling)
05

Safety considerations

EGFR inhibitors: rash, diarrhea, interstitial lung diseaseErbB2 inhibitors: cardiotoxicity, pulmonary toxicityOff-target effects, resistance mutations, efficacy loss by pathway feedback
06

Interacting drugs

erlotinib

10 more in the full profile.

07

Biomarkers

EGFR mutation or amplification status (especially in lung cancer)ErbB2 (HER2) protein overexpression/amplification (especially in breast, gastric cancer)ErbB4 fusions, expression levels—mainly research/experimental biomarkerPhosphorylation status for pathway activation

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