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Int. J. Mol. Sci. 2017, 18(11), 2420;

Molecular-Targeted Therapies for Epidermal Growth Factor Receptor and Its Resistance Mechanisms

Institute of Molecular Oncology, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan
Author to whom correspondence should be addressed.
Received: 20 October 2017 / Revised: 11 November 2017 / Accepted: 12 November 2017 / Published: 15 November 2017
(This article belongs to the Special Issue Kinase Signal Transduction 2017)
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Cancer therapies targeting epidermal growth factor receptor (EGFR), such as small-molecule kinase inhibitors and monoclonal antibodies, have been developed as standard therapies for several cancers, such as non-small cell lung cancer, colorectal cancer, pancreatic cancer, breast cancer, and squamous cell carcinoma of the head and neck. Although these therapies can significantly prolong progression-free survival, curative effects are not often achieved because of intrinsic and/or acquired resistance. The resistance mechanisms to EGFR-targeted therapies can be categorized as resistant gene mutations, activation of alternative pathways, phenotypic transformation, and resistance to apoptotic cell death. Analysis of the processes that modulate EGFR signal transduction by EGFR-targeted inhibitors, such as tyrosine kinase inhibitors and monoclonal antibodies, has revealed new therapeutic opportunities and has elucidated novel mechanisms contributing to the discovery of more effective anticancer treatments. In this review, we discuss the roles of EGFR in cancer development, therapeutic strategies for targeting EGFR, and resistance mechanisms to EGFR-targeted therapies, with a focus on cancer therapies for individual patients. View Full-Text
Keywords: epidermal growth factor receptor; resistance mechanisms; cancer epidermal growth factor receptor; resistance mechanisms; cancer

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Yamaoka, T.; Ohba, M.; Ohmori, T. Molecular-Targeted Therapies for Epidermal Growth Factor Receptor and Its Resistance Mechanisms. Int. J. Mol. Sci. 2017, 18, 2420.

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