Target intelligence / Profile preview

Receptor protein tyrosine kinase erbB‑2 (HER2)

Target
HER2
Molecular classification
Receptor, Enzyme, Transmembrane receptor tyrosine kinase, Human epidermal growth factor receptor (HER/EGFR/ERBB) family
01

Overview

Receptor protein tyrosine kinase erbB‑2 (HER2) is a transmembrane receptor tyrosine kinase belonging to the EGFR/HER/ErbB family. It does not bind a direct ligand but is activated through homo- or hetero-dimerization with other family members, leading to downstream signaling via MAPK, PI3K/Akt, and PKC pathways. HER2 plays a central role in cell proliferation and survival and is overexpressed in several cancers, making it an important therapeutic target.

Other names
ERBB2CD340Neu
02

Mechanism of action

Monoclonal antibodies bind to the extracellular domain, preventing dimerization and downstream signaling. Antibody-drug conjugates deliver cytotoxic payloads to HER2-expressing cells. Small molecule inhibitors block the intracellular kinase domain's activity, inhibiting phosphorylation and signaling.

03

Biological functions

Positive regulation of protein phosphorylationRegulation of transcriptionCell proliferationCell survivalCell differentiationAngiogenesis
04

Disease associations

Cancer
05

Safety considerations

Cardiotoxicity (associated with some HER2-targeted therapies)Resistance to therapyInfusion reactions
06

Interacting drugs

2 more in the full profile.

07

Biomarkers

HER2 amplificationHER2 overexpression

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