Target intelligence / Profile preview

Human Epidermal Growth Factor Receptor 1 (EGFR/HER1)

Target
EGFR/HER1
Molecular classification
Receptor, Receptor Tyrosine Kinase, Transmembrane receptor tyrosine kinase
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Overview

Human Epidermal Growth Factor Receptor 1 (EGFR/HER1) is a transmembrane receptor tyrosine kinase that plays a critical role in cell growth, proliferation, differentiation, and survival. Upon ligand binding, EGFR undergoes dimerization and autophosphorylation, leading to the activation of downstream signaling pathways such as RAS-RAF-MEK-ERK and PI3K-AKT. Aberrant EGFR signaling is frequently observed in various cancers, making it a key therapeutic target. Therapeutic strategies include monoclonal antibodies and small molecule inhibitors that block ligand binding or tyrosine kinase activity.

Other names
ErbB-1ERBB1Receptor tyrosine-protein kinase erbB-1Proto-oncogene c-ErbB-1
02

Mechanism of action

Inhibition of tyrosine kinase activity or ligand binding, leading to reduced downstream signaling.

03

Biological functions

Cell proliferationCell differentiationCell migrationCell survivalAnti-apoptosisGene expression regulationSignal transduction
04

Disease associations

CancerBreast cancerColorectal cancerNon-small cell lung cancerGlioblastomaAlzheimer’s diseaseAngina pectorisDiabetic foot ulcerIschemia
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Safety considerations

Resistance to EGFR inhibitorsSkin rashDiarrheaInterstitial lung disease
06

Interacting drugs

Monoclonal antibodies against the extracellular domain

1 more in the full profile.

07

Biomarkers

EGFR expression levels in tumor tissueEGFR mutation status

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