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.
Export Options
About this article
Cite this article as:
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 |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Combining Gene Therapy and Radiation Against Cancer
Current Gene Therapy Co-Expression and Purification of Recombinant Human Insulin-Like Growth Factor II and Insulin-Like Growth Factor Binding Protein-6 in Pichia pastoris Yeast
Protein & Peptide Letters Vitamin D and Asthma: Scientific Promise and Clinical Reality
Current Respiratory Medicine Reviews Sirtuins: Common Targets in Aging and in Neurodegeneration
Current Drug Targets Role of EGFR Inhibitors in the Treatment of Central Nervous System Metastases from Non-Small Cell Lung Cancer
Current Cancer Drug Targets On Epistasis: A Methodological Review for Detecting Gene-Gene Interactions Underlying Various Types of Phenotypic Traits
Recent Patents on Biotechnology Drug Repurposing Strategy against Fungal Biofilms
Current Topics in Medicinal Chemistry Targeting TNF-Alpha in HIV-1 Infection
Current Drug Targets Association of Hypothyroidism with Body Mass Index, Systolic Blood Pressure and Proteinuria in Diabetic Patients: Does treated Hypothyroidism with Thyroxine Replacement Therapy Prevent Nephropathy/Chronic Renal Disease?
Current Diabetes Reviews Targeted Drug Delivery to the Virus-Infected Airway; Complications and Remedies
Current Drug Delivery Pharmacokinetics of Biotech Drugs: Peptides, Proteins and Monoclonal Antibodies
Current Drug Metabolism Artesunate Enhances the Antiproliferative Effect of Temozolomide on U87MG and A172 Glioblastoma Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Telomere Maintenance as Therapeutic Target in Embryonal Tumours
Anti-Cancer Agents in Medicinal Chemistry Safety of Cabergoline in the Management of Pituitary Prolactin-Induced Symptoms with Patients Treated with Atypical Neuroleptics
Current Drug Safety The Role of Anticoagulation in Cancer Patients: Facts and Figures
Anti-Cancer Agents in Medicinal Chemistry Ability of Goat Milk to Modulate Healthy Human Peripheral Blood Lymphomonocyte and Polymorphonuclear Cell Function: In vitro Effects and Clinical Implications
Current Pharmaceutical Design Chemokines and Chemokine Receptors Blockers as New Drugs for the Treatment of Chronic Obstructive Pulmonary Disease
Current Medicinal Chemistry Role of Iodine, Selenium and Other Micronutrients in Thyroid Function and Disorders
Endocrine, Metabolic & Immune Disorders - Drug Targets Cancer Stem Cells – Are Surface Markers Alone Sufficient?
Current Stem Cell Research & Therapy Maternal Fibrinogen is Necessary for Embryonic Development
Current Drug Targets