Open Access
EGFR tyrosine kinases inhibitors in cancer treatment: in vitro and in vivo evidence
Anna Elisa Quatrale1,Letizia Porcelli1,Nicola Silvestris1,Giuseppe Colucci1,Angelo Angelo1,Amalia Azzariti1
Clinical Experimental Oncology Laboratory, National Cancer Institute Giovanni Paolo II, Via Hahnemann 10, 70126 Bari, Italy
DOI: 10.2741/3833 Volume 16 Issue 5, pp.1962-1972
Published: 01 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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Anna Elisa Quatrale, Letizia Porcelli, Nicola Silvestris, Giuseppe Colucci, Angelo Angelo, Amalia Azzariti. EGFR tyrosine kinases inhibitors in cancer treatment: in vitro and in vivo evidence. Frontiers in Bioscience-Landmark. 2011. 16(5); 1962-1972.