Abstract
Receptor tyrosine kinases play important roles in animal development and their deregulation has been linked to several pathologies, including cancer or diabetes. In cancer, the ERBB/HER family of receptors has been shown to participate in the pathophysiology of breast, gastric, colorectal, lung and head and neck tumors. Activation of HER receptors occurs by receptor-receptor interactions facilitated by ligand binding, overexpression or molecular alterations of the HER receptors. The best example is the known role of HER2 in the tumorigenesis of a proportion of breast tumors. In this review, we will describe the biological bases that govern HER receptor activation, and this will represent the bases for the explanation of how to target HER receptors in cancer. We will discuss the current therapeutic options to target HER receptors, which are based on anti-receptor antibodies or small molecule kinase inhibitors. We will also describe current clinical applications and future developments of agents which target HER receptors. Finally, we will mention mechanism of resistance to anti-HER therapies, and will describe options to overcome such resistances.
Keywords: HER receptors, kinase inhibitors, EGF ligands, targeted therapies, deregulation, cancer, diabetes, tumors, anti-receptor antibodies, resistances
Current Pharmaceutical Design
Title:Targeting HER Receptors in Cancer
Volume: 19 Issue: 5
Author(s): Alberto Ocana and Atanasio Pandiella
Affiliation:
Keywords: HER receptors, kinase inhibitors, EGF ligands, targeted therapies, deregulation, cancer, diabetes, tumors, anti-receptor antibodies, resistances
Abstract: Receptor tyrosine kinases play important roles in animal development and their deregulation has been linked to several pathologies, including cancer or diabetes. In cancer, the ERBB/HER family of receptors has been shown to participate in the pathophysiology of breast, gastric, colorectal, lung and head and neck tumors. Activation of HER receptors occurs by receptor-receptor interactions facilitated by ligand binding, overexpression or molecular alterations of the HER receptors. The best example is the known role of HER2 in the tumorigenesis of a proportion of breast tumors. In this review, we will describe the biological bases that govern HER receptor activation, and this will represent the bases for the explanation of how to target HER receptors in cancer. We will discuss the current therapeutic options to target HER receptors, which are based on anti-receptor antibodies or small molecule kinase inhibitors. We will also describe current clinical applications and future developments of agents which target HER receptors. Finally, we will mention mechanism of resistance to anti-HER therapies, and will describe options to overcome such resistances.
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Cite this article as:
Ocana Alberto and Pandiella Atanasio, Targeting HER Receptors in Cancer, Current Pharmaceutical Design 2013; 19 (5) . https://dx.doi.org/10.2174/1381612811306050808
DOI https://dx.doi.org/10.2174/1381612811306050808 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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