IMR Press / FBL / Volume 16 / Issue 5 / DOI: 10.2741/3833

Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on as a courtesy and upon agreement with Frontiers in Bioscience.


EGFR tyrosine kinases inhibitors in cancer treatment: in vitro and in vivo evidence

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1 Clinical Experimental Oncology Laboratory, National Cancer Institute Giovanni Paolo II, Via Hahnemann 10, 70126 Bari, Italy
2 Medical and Experimental Oncology Unit, National Cancer Institute Giovanni Paolo II, Via Hahnemann 10, 70126 Bari, Italy

Academic Editor: Amalia Azzariti

Front. Biosci. (Landmark Ed) 2011, 16(5), 1962–1972;
Published: 1 January 2011

The increasing understanding of the molecular mechanisms of neoplastic transformation and progression has prompted the search for novel drugs that could interfere with the intracellular targets involved in this process. EGFR is implicated in the development and progression of the majority of the common human epithelial cancer; therefore different agents have been developed to block EGFR activation in cancer cells. This review focuses on EGFR-tyrosine kinase inhibitors in clinical practice that interfere with ATP binding, inhibiting tyrosine kinase activity and subsequently blocking signal transduction from EGFR. We report current knowledge on molecular mechanisms underlying the anticancer activity of EGFR-tyrosine kinase inhibitors in preclinical models, with particular attention to EGFR downstream effectors responsible for treatment efficacy or resistance.

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