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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors

Author(s): C. Wang, H. Gao, J. Dong, F. Wang, P. Li and J. Zhang

Volume 21, Issue 11, 2014

Page: [1336 - 1350] Pages: 15

DOI: 10.2174/0929867320666131119124646

Price: $65


Dysregulation of receptor tyrosine kinases (RTKs) in cancer cells is extremely common. Overexpression of human epidermal growth factor receptor (EGFR/HER) tyrosine kinase is correlated with tumor aetiology, progression and poor prognosis. Their activation is also observed frequently in human cancers. Therefore, RTKs have been identified as important therapeutic targets in oncology. Many therapeutic methods have been developed based on inhibition of EGFR and HER-2. Herein, we will discuss recent progress in the development of EGFR/HER-2 tyrosine kinase inhibitors. We will focus on the design strategies, pharmacological profiles and structure-activity relationships (SARs) of EGFR and HER-2 inhibitors.

Keywords: EGFR, ERBB, HER-2, structure-activity relationship, tyrosine kinase.

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