Epidermal growth factor receptor family (ErbB family) (ErbB family)

The Epidermal Growth Factor Receptor (EGFR) family, also known as the ErbB or HER family, consists of four transmembrane receptor tyrosine kinases: EGFR (ErbB1), HER2 (ErbB2), HER3 (ErbB3), and HER4 (ErbB4) [1, 8, 12]. These receptors play a fundamental role in cell signaling, governing processes such as proliferation, survival, and differentiation by activating the Ras/MAPK and PI3K/Akt pathways [1, 3, 10]. In many cancers, these receptors are overexpressed or mutated, leading to uncontrolled cell growth and therapeutic resistance [1, 16, 18]. While EGFR and HER2 have long been primary targets for oncology drugs, HER3 is increasingly recognized for its role in mediating resistance to EGFR and HER2 inhibitors through its potent activation of the PI3K pathway [7, 11, 13, 17]. Consequently, therapeutic development has shifted toward pan-HER inhibitors and multi-target agents that can simultaneously block multiple family members to overcome compensatory signaling and improve patient outcomes [2, 5, 6, 9].

Other names

ErbB familyHER familyHuman epidermal growth factor receptor familyErbB receptor tyrosine kinases

Inhibition of intracellular tyrosine kinase activity through competitive or irreversible ATP-binding [3, 6, 9], and monoclonal antibody-mediated blockade of extracellular ligand binding or receptor dimerization [11, 14, 15].