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Insight into the medicinal chemistry of EGFR and HER-2 inhibitors

C Wang, H Gao, J Dong

  • 1School of Medicine, Xi'an Jiaotong University, No. 76, Yanta West Road, 710061, Xi'an, ShaanXi Province, P.R. China. zhj8623@mail.xjtu.edu.cn.

Current Medicinal Chemistry
|November 21, 2013
PubMed

Insights

Receptor tyrosine kinases (RTKs) are common in cancer. This review covers new EGFR/HER-2 tyrosine kinase inhibitors, focusing on design, pharmacology, and structure-activity relationships for cancer therapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Dysregulation of receptor tyrosine kinases (RTKs) is prevalent in cancer.
  • Overexpression and activation of human epidermal growth factor receptor (EGFR/HER) tyrosine kinase correlate with tumor progression and poor prognosis.
  • RTKs are critical therapeutic targets in oncology.

Purpose of the Study:

  • To review recent advancements in the development of EGFR/HER-2 tyrosine kinase inhibitors.
  • To focus on design strategies, pharmacological profiles, and structure-activity relationships (SARs) of these inhibitors.

Main Methods:

  • Literature review of recent progress in EGFR/HER-2 tyrosine kinase inhibitor development.
  • Analysis of design strategies, pharmacological profiles, and SARs.

Main Results:

  • Recent progress has been made in developing novel EGFR/HER-2 tyrosine kinase inhibitors.
  • Understanding of design strategies, pharmacological profiles, and SARs is crucial for effective drug development.

Conclusions:

  • EGFR/HER-2 tyrosine kinase inhibitors represent a promising therapeutic strategy for various cancers.
  • Continued research into inhibitor design and SARs will enhance their clinical efficacy.

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