Target intelligence / Profile preview

ErbB receptor family (ErbB family)

Target
ErbB family
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor
01

Overview

The ErbB receptor family, also known as the epidermal growth factor receptor (EGFR) or HER family, consists of four closely related type I receptor tyrosine kinases: EGFR (ErbB1), HER2 (ErbB2), HER3 (ErbB3), and HER4 (ErbB4) (Wikipedia, 2024; UniProt, 2024). These receptors play a critical role in regulating essential cellular processes, including growth, proliferation, differentiation, and survival, through the activation of downstream signaling pathways such as MAPK/ERK and PI3K/Akt (NIH, 2024). Dysregulation of ErbB signaling, often through gene amplification, overexpression, or activating mutations, is a hallmark of various malignancies, including non-small cell lung cancer, breast cancer, and colorectal cancer (PubMed, 2023). Consequently, this family has become a primary focus for targeted cancer therapies, leading to the development of small-molecule tyrosine kinase inhibitors (TKIs) and monoclonal antibodies (StatPearls, 2024). While these therapies have significantly improved patient outcomes, challenges such as acquired resistance and off-target toxicities like skin rash and cardiotoxicity remain significant clinical hurdles (NIH, 2024).

Other names
Epidermal growth factor receptor familyHER familyType I receptor tyrosine kinase family
02

Mechanism of action

Small molecule inhibition of the intracellular tyrosine kinase domain and monoclonal antibody-mediated blockade of extracellular ligand binding or receptor dimerization.

03

Biological functions

Signal transductionCell proliferationCell survivalCell differentiationCell migration
04

Disease associations

Cancer
05

Safety considerations

Acneiform skin rashDiarrheaCardiotoxicity (LVEF decrease)Interstitial lung disease
06

Interacting drugs

11 more in the full profile.

07

Biomarkers

EGFR mutation statusHER2 amplification/overexpressionKRAS/NRAS mutation status

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