title: EGFR tyrosine kinases inhibitors in cancer treatment: in vitro and in vivo evidence.
abstract: 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.
authors.affiliation: Clinical Experimental Oncology Laboratory, National Cancer Institute Giovanni Paolo II, Via Hahnemann 10, 70126 Bari, Italy.
authors.forename: Anna Elisa
authors.initials: AE
authors.lastname: Quatrale
authors.forename: Letizia
authors.initials: L
authors.lastname: Porcelli
authors.forename: Nicola
authors.initials: N
authors.lastname: Silvestris
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Colucci
authors.forename: Angelo
authors.initials: A
authors.lastname: Angelo
authors.forename: Amalia
authors.initials: A
authors.lastname: Azzariti
mesh_terms: D000970:Antineoplastic Agents / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D002455:Cell Division / Q000187:drug effects; D066246:ErbB Receptors / Q000037:antagonists & inhibitors / Q000502:physiology; D000069347:Erlotinib Hydrochloride; D000077156:Gefitinib; D006801:Humans; D000077341:Lapatinib; D009361:Neoplasm Invasiveness / Q000517:prevention & control; D009362:Neoplasm Metastasis / Q000188:drug therapy; D009369:Neoplasms / Q000188:drug therapy*; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D011799:Quinazolines / Q000627:therapeutic use*; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D000077341:Lapatinib; D000069347:Erlotinib Hydrochloride; D066246:ErbB Receptors; D011505:Protein-Tyrosine Kinases; D000077156:Gefitinib