Target intelligence / Profile preview

Human Epidermal Growth Factor Receptor (HER)

Target
HER
Molecular classification
Receptor, Receptor Tyrosine Kinase
01

Overview

The Human Epidermal Growth Factor Receptor (HER) family, also known as the ErbB family, comprises four closely related receptor tyrosine kinases: EGFR/ErbB1/HER1, HER2/ErbB2, HER3/ErbB3, and HER4/ErbB4. These receptors play critical roles in regulating cell growth, survival, differentiation, and migration. Activation occurs primarily through dimerization—either as homodimers or heterodimers—between two HER family members. This process is often triggered by extracellular ligands such as epidermal growth factor or neuregulins. Dimerization leads to transphosphorylation of intracellular domains on specific tyrosines, initiating multiple downstream signaling cascades that regulate cellular processes. Dysregulation—such as overexpression or mutation—is implicated in various cancers including breast cancer where amplification of the HER2 gene drives aggressive tumor behavior and serves as an important therapeutic target.

Other names
ErbB familyErbB1HER1EGFRErbB2HER2ErbB3HER3ErbB4HER4
02

Mechanism of action

Inhibition of HER receptor tyrosine kinase activity, blocking downstream signaling pathways such as MAPK and PI3K/AKT.

03

Biological functions

Cell growthCell survivalCell differentiationCell migrationSignal transductionCell proliferation
04

Disease associations

Cancer
05

Safety considerations

Drug resistanceCardiac dysfunctionDiarrhea
06

Biomarkers

HER2 gene amplificationHER2 protein overexpression

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