![conference banner](/images/conference-banner.jpeg)
Abstract
The inherited or acquired deregulation of protein kinase activity has been implicated in the pathogenesis of many human diseases, including cancer. Therefore, the inhibition of kinases has been proposed to be a promising strategy in the context of anti-cancer treatment. Many other kinases have been selected as drug discovery targets based on the prevalence of mutations, over-expression and unscheduled activation in human cancer. Of the various protein kinases chosen, Src family kinases are amongst the most extensively studied kinase oncogenes in academia and industry. This review focuses on our current understanding of the deregulation and role of Src family kinases in human cancer and leukemia. Recent data implicate the action of c-Src in cancer metastasis, mediated by up-regulation of various protease systems (calpain, uPA) as well as disruption of E-cadherin signalling. Moreover, novel roles of various Src family members in the development of human leukemia have been found. New insights into downstream signalling mechanisms, including the activation of STAT3, PDK1 and Akt, further corroborate the importance of Src family kinases in tumorigenesis and chemoresistance. Despite our rather clear understanding of Src family kinases as pro-oncogenes no Src family kinase inhibitor has entered a clinical trial so far. This review will discuss prerequisites to be fulfilled for clinically targeting c-Src and its homologues using small molecule drugs.
Keywords: protein kinases, src family kinases, small molecule kinase inhibitor, leukemogenesis, cancerogenesis
Current Pharmaceutical Design
Title: Src Family Kinases: Potential Targets for the Treatment of Human Cancer and Leukemia
Volume: 9 Issue: 25
Author(s): Markus Warmuth, Robert Damoiseaux, Yi Liu, Doriano Fabbro and Nathanael Gray
Affiliation:
Keywords: protein kinases, src family kinases, small molecule kinase inhibitor, leukemogenesis, cancerogenesis
Abstract: The inherited or acquired deregulation of protein kinase activity has been implicated in the pathogenesis of many human diseases, including cancer. Therefore, the inhibition of kinases has been proposed to be a promising strategy in the context of anti-cancer treatment. Many other kinases have been selected as drug discovery targets based on the prevalence of mutations, over-expression and unscheduled activation in human cancer. Of the various protein kinases chosen, Src family kinases are amongst the most extensively studied kinase oncogenes in academia and industry. This review focuses on our current understanding of the deregulation and role of Src family kinases in human cancer and leukemia. Recent data implicate the action of c-Src in cancer metastasis, mediated by up-regulation of various protease systems (calpain, uPA) as well as disruption of E-cadherin signalling. Moreover, novel roles of various Src family members in the development of human leukemia have been found. New insights into downstream signalling mechanisms, including the activation of STAT3, PDK1 and Akt, further corroborate the importance of Src family kinases in tumorigenesis and chemoresistance. Despite our rather clear understanding of Src family kinases as pro-oncogenes no Src family kinase inhibitor has entered a clinical trial so far. This review will discuss prerequisites to be fulfilled for clinically targeting c-Src and its homologues using small molecule drugs.
Export Options
About this article
Cite this article as:
Warmuth Markus, Damoiseaux Robert, Liu Yi, Fabbro Doriano and Gray Nathanael, Src Family Kinases: Potential Targets for the Treatment of Human Cancer and Leukemia, Current Pharmaceutical Design 2003; 9 (25) . https://dx.doi.org/10.2174/1381612033454126
DOI https://dx.doi.org/10.2174/1381612033454126 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
Blood-based biomarkers in large-scale screening for neurodegenerative diseases
Disease biomarkers are necessary tools that can be employ in several clinical context of use (COU), ranging from the (early) diagnosis, prognosis, prediction, to monitor of disease state and/or drug efficacy. Regarding neurodegenerative diseases, in particular Alzheimer’s disease (AD), a battery of well-validated biomarkers are available, such as cerebrospinal fluid ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Diabetes mellitus: advances in diagnosis and treatment driving by precision medicine
Diabetes mellitus (DM) is a chronic degenerative metabolic disease with ever increasing prevalence worldwide which is now an epidemic disease affecting 500 million people worldwide. Insufficient insulin secretion from pancreatic β cells unable to maintain blood glucose homeostasis is the main feature of this disease. Multifactorial and complex nature of ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Caffeic Acid, A Versatile Pharmacophore: An Overview
Mini-Reviews in Medicinal Chemistry Computational Peptidology: A New and Promising Approach to Therapeutic Peptide Design
Current Medicinal Chemistry In Silico Identification and Analysis of Drug Resistant Mutants of ABL Tyrosine Kinase Based on Detrimental Missense Mutations
Current Signal Transduction Therapy Self-Adjuvanting Lipopeptide Vaccines
Current Medicinal Chemistry Aurora A and B Kinases - Targets of Novel Anticancer Drugs
Recent Patents on Anti-Cancer Drug Discovery Melanoma Immunotherapy: Past, Present, and Future
Current Pharmaceutical Design Aminophosphonate Metal Complexes of Biomedical Potential
Current Medicinal Chemistry Serum Proteomics in the Diagnosis and Treatment of Haematological Malignancies
Current Proteomics Toll Like Receptors Signaling Pathways as a Target for Therapeutic Interventions
Current Signal Transduction Therapy Therapeutic Potential of Inhibiting Brutons Tyrosine Kinase, (BTK)
Current Pharmaceutical Design RNA Silencing: Recent Developments on miRNAs
Recent Patents on DNA & Gene Sequences Targeting Transcription Factor Binding to DNA by Competing with DNA Binders as an Approach for Controlling Gene Expression
Current Topics in Medicinal Chemistry Cytosine Methyltransferases as Tumor Markers
Current Genomics Role of Cerium Oxide Nanoparticles and Doxorubicin in Improving Cancer Management: A Mini Review
Current Pharmaceutical Design Genetic Polymorphism and Tumor Immunotherapy
Current Pharmacogenomics siRNA-Mediated Knock-Down of P-Glycoprotein Expression Reveals Distinct Cellular Disposition of Anticancer Tyrosine Kinases Inhibitors
Drug Metabolism Letters Emerging Treatments in Acute Lymphoblastic Leukemia
Current Cancer Drug Targets Use of Intravenous Immunoglobulin in the Treatment of Immune-Mediated Demyelinating Diseases of the Nervous System
Current Pharmaceutical Design Marizomib, a Proteasome Inhibitor for All Seasons: Preclinical Profile and a Framework for Clinical Trials
Current Cancer Drug Targets Nuclear Receptor SHP as a Potential Therapeutic Target for Liver Cancer
Current Cancer Therapy Reviews