Abstract
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.
Current Medicinal Chemistry
Title:Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors
Volume: 21 Issue: 11
Author(s): C. Wang, H. Gao, J. Dong, F. Wang, P. Li and J. Zhang
Affiliation:
Keywords: EGFR, ERBB, HER-2, structure-activity relationship, tyrosine kinase.
Abstract: 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.
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Cite this article as:
Wang C., Gao H., Dong J., Wang F., Li P. and Zhang J., Insight into the Medicinal Chemistry of EGFR and HER-2 Inhibitors, Current Medicinal Chemistry 2014; 21 (11) . https://dx.doi.org/10.2174/0929867320666131119124646
DOI https://dx.doi.org/10.2174/0929867320666131119124646 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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