![]() These receptors are physiologically expressed in epithelial, mesenchymal, cardiac, and neuronal tissues. In mammals, four ErbB/HER receptors have been described: the epidermal growth factor receptor (EGFR/HER1), HER2/ErbB2/neu, HER3/ErbB3, and HER4/ErbB4. ![]() The ErbB/HER receptor tyrosine kinases (RTK) play critical roles in animal development, and their altered function may contribute to the pathophysiological development of certain types of tumors. Here we discuss the state of the art of the preclinical and clinical development of drugs aimed at targeting HER3 with therapeutic purposes. In addition, the use of aptamers specifically interacting with HER3, vaccines or HER3-targeting siRNAs have also been developed. The most abundant are antibodies or engineered antibody derivatives that specifically recognize the extracellular region of HER3. Two types of agents targeting HER3 have been developed. Because of those circumstances, efforts to develop and test agents targeting HER3 have been carried out. In addition, HER3 has been associated to resistance to some chemotherapeutic drugs. Furthermore, expression and activation of HER3 has been linked to resistance to drugs that target other HER receptors such as agents that act on EGFR or HER2. ![]() That fact, together with the role of HER3 in promoting cell proliferation, implicate that targeting HER3 may have therapeutic relevance. ![]() The HER3 protein, that belongs to the ErbB/HER receptor tyrosine kinase (RTK) family, is expressed in several types of tumors.
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