Targeting HER receptors in cancer
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Published on: June 13, 2014
Alberto Ocaña1, Atanasio Pandiella
1Instituto de Biologia Molecular y Celular del Cancer-CIC, Campus Miguel de Unamuno, 37007- Salamanca, Spain.
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.
Insights
This review explains how human epidermal growth factor receptor (HER) activation drives cancer and discusses targeted therapies. It covers current treatments, future developments, and strategies to overcome resistance to anti-HER therapies.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Receptor tyrosine kinases (RTKs) are crucial in development; their dysregulation links to diseases like cancer and diabetes.
- The ERBB/HER family of receptors is implicated in various cancers, including breast, gastric, colorectal, lung, and head and neck tumors.
- HER receptor activation involves receptor-receptor interactions, ligand binding, overexpression, or molecular alterations, with HER2 being a key example in breast cancer.
Purpose of the Study:
- To elucidate the biological mechanisms of HER receptor activation.
- To provide a foundation for understanding how to target HER receptors therapeutically in cancer.
- To review current and future strategies for targeting HER receptors and overcoming resistance.
Main Methods:
- Literature review of biological bases governing HER receptor activation.
- Analysis of current therapeutic options targeting HER receptors, including antibodies and kinase inhibitors.
- Examination of clinical applications, future developments, and resistance mechanisms.
Main Results:
- Detailed explanation of HER receptor activation pathways.
- Overview of existing anti-HER therapies (antibodies, small molecule inhibitors).
- Discussion of clinical efficacy, emerging treatments, and resistance patterns.
Conclusions:
- Targeting HER receptors is a validated strategy in oncology.
- Understanding activation mechanisms is key to developing effective therapies.
- Addressing resistance is crucial for improving patient outcomes in HER-targeted cancer treatment.
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