Abstract
Fyn is a non-receptor tyrosine kinase belonging to the Src family kinases. It has been shown to play important roles in neuronal functions, including myelination and oligodendrocytes formation, and in inflammatory processes. It has also demonstrated its involvement in signaling pathways that lead to severe brain pathologies, such as Alzheimers and Parkinsons diseases. Moreover, Fyn is upregulated in some malignancies. Experimental studies demonstrated that Fyn inhibition could be useful in the disruption of metabolic processes involved in cancer and in neurodegenerative diseases. Unfortunately no specific Fyn inhibitor has been discovered so far, being the reported compounds active also on other members of Src family or on different tyrosine kinases. However, multitargeted inhibitors might be endowed with therapeutic potential. Indeed, as increasingly reported, also a not completely selective inhibitor of a specific protein could be therapeutically useful, affecting a number of cell pathways involved especially in cancer development. In this review, we report some examples of small molecule tyrosine kinase inhibitors for which data on Fyn inhibition, both in enzymatic and in cell assays, have been reported, with the aim of giving information as starting point for the researchers working in this field.
Keywords: Fyn, Src, tyrosine kinase, Alzheimer's disease, brain, cancer, inhibitors
Current Medicinal Chemistry
Title: Fyn Kinase in Brain Diseases and Cancer: The Search for Inhibitors
Volume: 18 Issue: 19
Author(s): S. Schenone, C. Brullo, F. Musumeci, M. Biava, F. Falchi and M. Botta
Affiliation:
Keywords: Fyn, Src, tyrosine kinase, Alzheimer's disease, brain, cancer, inhibitors
Abstract: Fyn is a non-receptor tyrosine kinase belonging to the Src family kinases. It has been shown to play important roles in neuronal functions, including myelination and oligodendrocytes formation, and in inflammatory processes. It has also demonstrated its involvement in signaling pathways that lead to severe brain pathologies, such as Alzheimers and Parkinsons diseases. Moreover, Fyn is upregulated in some malignancies. Experimental studies demonstrated that Fyn inhibition could be useful in the disruption of metabolic processes involved in cancer and in neurodegenerative diseases. Unfortunately no specific Fyn inhibitor has been discovered so far, being the reported compounds active also on other members of Src family or on different tyrosine kinases. However, multitargeted inhibitors might be endowed with therapeutic potential. Indeed, as increasingly reported, also a not completely selective inhibitor of a specific protein could be therapeutically useful, affecting a number of cell pathways involved especially in cancer development. In this review, we report some examples of small molecule tyrosine kinase inhibitors for which data on Fyn inhibition, both in enzymatic and in cell assays, have been reported, with the aim of giving information as starting point for the researchers working in this field.
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Schenone S., Brullo C., Musumeci F., Biava M., Falchi F. and Botta M., Fyn Kinase in Brain Diseases and Cancer: The Search for Inhibitors, Current Medicinal Chemistry 2011; 18 (19) . https://dx.doi.org/10.2174/092986711796150531
DOI https://dx.doi.org/10.2174/092986711796150531 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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