title: Insight into the medicinal chemistry of EGFR and HER-2 inhibitors.
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.
authors.forename: C
authors.initials: C
authors.lastname: Wang
authors.forename: H
authors.initials: H
authors.lastname: Gao
authors.forename: J
authors.initials: J
authors.lastname: Dong
authors.forename: F
authors.initials: F
authors.lastname: Wang
authors.forename: P
authors.initials: P
authors.lastname: Li
authors.affiliation: School of Medicine, Xi'an Jiaotong University, No. 76, Yanta West Road, 710061, Xi'an, ShaanXi Province, P.R. China. zhj8623@mail.xjtu.edu.cn.
authors.forename: J
authors.initials: J
authors.lastname: Zhang
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000627:therapeutic use; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000627:therapeutic use*; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D066246:ErbB Receptors; D047428:Protein Kinase Inhibitors; D018719:Erb-b2 Receptor Tyrosine Kinases