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Erb-B2 receptor tyrosine kinase 3 (ERBB3), also known as HER3, is a member of the epidermal growth factor receptor family. Unlike other members, it has impaired intrinsic kinase activity but plays a critical role in signal transduction by forming heterodimers—most notably with HER2/ErbB2—to activate downstream pathways involved in cell proliferation and survival. It is widely expressed during development and adulthood across various tissues including skin, nervous system, heart, lungs, gastrointestinal tract, reproductive system, urinary tract, and endocrine organs. Dysregulation or mutation of ERBB3 contributes significantly to carcinogenesis and drug resistance mechanisms in multiple human cancers. As such, it is an important therapeutic target under investigation for novel cancer treatments using monoclonal antibodies or antibody-drug conjugates designed specifically against this molecule.
Drugs targeting ERBB3 typically act by one or more of the following mechanisms: Inhibition of ligand binding to prevent activation/dimerization; Disruption of heterodimer formation with other ErbB receptors (especially HER2/ERBB2); Antibody-drug conjugates delivering cytotoxic payloads to cells expressing high levels of ERBB3.
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