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Current Pharmaceutical Design


ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Targeting the EGFR-family for Therapy: Biological Challenges and Clinical Perspective

Author(s): Rachana Patel and Hing Y. Leung

Volume 18 , Issue 19 , 2012

Page: [2672 - 2679] Pages: 8

DOI: 10.2174/138161212800626148

Price: $65


Members of epidermal growth factor receptor (EGFR) or ErbB receptor family play a critical role in a wide range of human cancers. In the past decade, there has been a remarkable progress in developing ErbB targeted therapeutics. However, a substantial portion of patients has non-responsive disease or subsequently shows evidence of tumour relapse following initial success with anti-ErbB agents. Improved insights into the biology of ErbB receptor family have led to more effective second- and third-generation anti-ErbB therapies. In this review, we have summarised salient features of the ErbB receptor physiology and highlighted key mechanisms involved in abnormal ErbB signalling in tumorigenesis. The rationale of anti-ErbB receptor therapies are outlined along with key mechanisms proposed for resistance to treatment as well as the current concept of combined anti-ErbB therapies. In conclusion, improved understanding of the molecular pathways that confer resistance to anti-ErbB therapeutics will be essential in minimising tumour resistance to ErbB targeted treatments.

Keywords: EGFR, ErbB, receptor tyrosine kinase, monoclonal antibodies, small molecule inhibitors, cancers, tumorigenesis, tumour resistance, dimerization, gene amplifications

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