Abstract
Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinase signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of several neoplasms, including lung, breast, kidney and pancreatic cancer as well as gastro-intestinal stromal tumors and chronic myeloid leukemia. This comprehensive review focuses on the most relevant members of the first and the second generation TKIs designed to interact with receptor and nonreceptor TKs. Attention is mainly focused on molecular mechanisms in in vitro and in vivo models related to the clinical activity of the drugs and to the development of resistance to treatment, still the major challenge in cancer research and care.
Keywords: Angiogenesis, HER family, multitarget, nonreceptors, receptors, resistance, tyrosine kinase inhibitors
Current Cancer Drug Targets
Title: Tyrosine Kinase Inhibitors
Volume: 10 Issue: 5
Author(s): C. Natoli, B. Perrucci, F. Perrotti, L. Falchi and S. Iacobelli
Affiliation:
Keywords: Angiogenesis, HER family, multitarget, nonreceptors, receptors, resistance, tyrosine kinase inhibitors
Abstract: Over the last ten years, several new and therapeutically relevant cancer drugs targeting tyrosine kinase signaling pathways have been developed. Tyrosine kinase inhibitors (TKIs) are a pharmaceutical class of small molecules, orally available, well-tolerated, worldwide approved drugs for the treatment of several neoplasms, including lung, breast, kidney and pancreatic cancer as well as gastro-intestinal stromal tumors and chronic myeloid leukemia. This comprehensive review focuses on the most relevant members of the first and the second generation TKIs designed to interact with receptor and nonreceptor TKs. Attention is mainly focused on molecular mechanisms in in vitro and in vivo models related to the clinical activity of the drugs and to the development of resistance to treatment, still the major challenge in cancer research and care.
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Cite this article as:
Natoli C., Perrucci B., Perrotti F., Falchi L. and Iacobelli S., Tyrosine Kinase Inhibitors, Current Cancer Drug Targets 2010; 10 (5) . https://dx.doi.org/10.2174/156800910791517208
DOI https://dx.doi.org/10.2174/156800910791517208 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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