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Target intelligence / Profile preview
Human Epidermal Growth Factor Receptor 2 (HER2)
- Target
- HER2
- Molecular classification
- Receptor, Transmembrane receptor, Tyrosine kinase receptor, HER family
01
Overview
HER2 (ERBB2) is a transmembrane tyrosine kinase receptor that is part of the human epidermal growth factor receptor (HER) family. Overexpression or amplification of the HER2 gene is observed in several cancer types, leading to increased cell proliferation, survival, invasion, and metastasis. HER2 is a validated therapeutic target, with several approved therapies that have significantly improved outcomes for patients with HER2-positive cancers.
- Other names
- ERBB2HER2/neu
02
Mechanism of action
Monoclonal antibodies bind to the extracellular domain of HER2, inhibiting downstream signaling. Tyrosine kinase inhibitors block the intracellular kinase domain, preventing phosphorylation and activation of downstream pathways. Antibody-drug conjugates deliver cytotoxic agents to HER2-expressing cells.
03
Biological functions
Cell proliferationCell survivalSignal transductionRegulation of cell growthBreast tissue development
04
Disease associations
CancerBreast cancerGastric cancerGallbladder cancerOvarian cancerEndometrial cancerEsophageal cancer
05
Safety considerations
Cardiotoxicity (trastuzumab)Resistance to therapyAdverse effects associated with specific tyrosine kinase inhibitors and antibody-drug conjugates
06
Interacting drugs
4 more in the full profile.
07
Biomarkers
HER2 protein overexpression (IHC)ERBB2 gene amplification (FISH)
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