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