Target intelligence / Profile preview

Human Epidermal Growth Factor Receptor 2 Tyrosine Kinase Domain (HER2 TKD)

Target
HER2 TKD
Molecular classification
Receptor Tyrosine Kinase, Enzyme, Protein Kinase, Tyrosine Kinase
01

Overview

The Human Epidermal Growth Factor Receptor 2 (HER2) Tyrosine Kinase Domain is the intracellular catalytic domain of the HER2 receptor, a transmembrane tyrosine kinase receptor involved in cell growth, survival, and differentiation. It is activated by dimerization, leading to autophosphorylation and downstream signaling through the MAPK and PI3K/AKT pathways. HER2 overexpression or amplification is implicated in various cancers, making it a key therapeutic target. Unlike other HER family members, HER2 does not directly bind ligands, instead relying on dimerization for activation.

Other names
ErbB2 Tyrosine Kinase DomainCD340 Tyrosine Kinase DomainNeu Tyrosine Kinase Domain
02

Mechanism of action

Inhibition of tyrosine kinase activity, Antibody-dependent cell-mediated cytotoxicity (ADCC)

03

Biological functions

Signal transductionCell growthCell survivalCell differentiationCell proliferationAutophosphorylation
04

Disease associations

CancerBreast cancerGastric cancerGastroesophageal cancerOvarian cancerEndometrial cancerBladder cancerLung cancerColon cancer
05

Safety considerations

CardiotoxicityInfusion-related reactionsDiarrhea (with tyrosine kinase inhibitors)Off-target effects on EGFR and other kinases
06

Interacting drugs

Lapatinib

2 more in the full profile.

07

Biomarkers

HER2 amplificationHER2 overexpression

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