Tyrosine kinase inhibitors - Small molecular weight compounds Inhibiting EGFR

Bálint Hegymegi-Barakonyi, Dániel Eros, Csaba Szántai-Kis, Nóra Breza, Péter Bánhegyi, Gábor Viktor Szabó, Edit Várkondi, István Peták, László Orfi, György Kéri

Research output: Contribution to journalReview article

19 Citations (Scopus)


Abnormally elevated EGFR kinase activity can lead to various pathological states, including proliferative diseases such as cancer. The development of selective protein kinase inhibitors has become an important area of drug discovery for the potential treatment of a variety of solid tumors such as breast, ovarian and colorectal cancers, NSCLC, and carcinoma of the head and neck. There are three small molecule EGFR kinase inhibitor drugs in clinical use (gefitinib, erlotinib and lapatinib), and several others are currently undergoing clinical development. This review summarizes the development of EGFR kinase inhibitors, and includes descriptions of the binding modes, the importance of a multiple-targets strategy, the effects of sensitizing and resistance mutations in the EGFR, and molecular diagnostic approaches. In addition, the use of target fishing for selectivity profiling, off-target identification and quantitative structure-activity relationship modeling for the prediction of EGFR inhibition is discussed.

Original languageEnglish
Pages (from-to)308-321
Number of pages14
JournalCurrent Opinion in Molecular Therapeutics
Issue number3
Publication statusPublished - Jun 1 2009


  • EGFR
  • EGFR kinase inhibitor
  • Multiple targets
  • Signal transduction

ASJC Scopus subject areas

  • Molecular Medicine
  • Molecular Biology
  • Genetics
  • Pharmacology
  • Drug Discovery
  • Genetics(clinical)

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  • Cite this

    Hegymegi-Barakonyi, B., Eros, D., Szántai-Kis, C., Breza, N., Bánhegyi, P., Szabó, G. V., Várkondi, E., Peták, I., Orfi, L., & Kéri, G. (2009). Tyrosine kinase inhibitors - Small molecular weight compounds Inhibiting EGFR. Current Opinion in Molecular Therapeutics, 11(3), 308-321.