Abstract
The need for novel approaches for targeting well-known protein families in drug discovery has been discussed for several years. There is a huge amount of literature on the inhibition of kinases with small molecules targeting the ATP site, and as a result of this extensive research, there are a large number of kinase inhibitors in the clinic. However, even though the idea of targeting other sites on kinases is not new, relatively little has been reported. In this review we give an overview of structurally characterized allosteric kinase inhibitors, outline the benefits of these with the use of case studies and then discuss the challenges that need to be overcome and the opportunities for doing this.
Keywords: Activator, Allosteric, Binding mode, Inhibitor, Kinase, Structure-Based Drug Discovery, Target Space.
Current Topics in Medicinal Chemistry
Title:Expanding the Opportunities for Modulating Kinase Targets with Allosteric Approaches
Volume: 17 Issue: 1
Author(s): Henrik Mobitz, Wolfgang Jahnke and Sandra W. Cowan-Jacob
Affiliation:
Keywords: Activator, Allosteric, Binding mode, Inhibitor, Kinase, Structure-Based Drug Discovery, Target Space.
Abstract: The need for novel approaches for targeting well-known protein families in drug discovery has been discussed for several years. There is a huge amount of literature on the inhibition of kinases with small molecules targeting the ATP site, and as a result of this extensive research, there are a large number of kinase inhibitors in the clinic. However, even though the idea of targeting other sites on kinases is not new, relatively little has been reported. In this review we give an overview of structurally characterized allosteric kinase inhibitors, outline the benefits of these with the use of case studies and then discuss the challenges that need to be overcome and the opportunities for doing this.
Export Options
About this article
Cite this article as:
Mobitz Henrik, Jahnke Wolfgang and Cowan-Jacob W. Sandra, Expanding the Opportunities for Modulating Kinase Targets with Allosteric Approaches, Current Topics in Medicinal Chemistry 2017; 17 (1) . https://dx.doi.org/10.2174/1568026616666160719165314
DOI https://dx.doi.org/10.2174/1568026616666160719165314 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Gold and Silver Nanoparticles for Applications in Theranostics
Current Topics in Medicinal Chemistry Cancer/Testis Antigens Trigger Epithelial-Mesenchymal Transition and Genesis of Cancer Stem-Like Cells
Current Pharmaceutical Design Immunoregulatory and Effector Activities of Nitric Oxide and Reactive Nitrogen Species in Cancer
Current Medicinal Chemistry C-11 Radiochemistry in Cancer Imaging Applications
Current Topics in Medicinal Chemistry Controlled Gene Delivery Can Enhance Therapeutic Outcome for Cancer Immune Therapy for Melanoma
Current Gene Therapy The Fate of Nanocarriers As Nanomedicines In Vivo: Important Considerations and Biological Barriers to Overcome
Current Medicinal Chemistry Novel VEGF-independent Strategies Targeting Tumor Vasculature: Clinical Aspects
Current Pharmaceutical Design Mechanisms of Tubulin Binding Ligands to Target Cancer Cells: Updates on their Therapeutic Potential and Clinical Trials
Current Cancer Drug Targets Phytosterols in Cancer: From Molecular Mechanisms to Preventive and Therapeutic Potentials
Current Medicinal Chemistry Molecular Phenotyping of Mouse Mutant Resources by RNA Expression Profiling
Current Genomics Fucose Specific Lectins in Cancer Research and Diagnosis
Drug Design Reviews - Online (Discontinued) Tumor Angiogenesis and VEGFR-2: Mechanism, Pathways and Current Biological Therapeutic Interventions
Current Drug Metabolism Development of Patents and Clinical Trials on Regenerative Therapy: Gene Therapy
Recent Patents on Regenerative Medicine Archaeosome Immunostimulatory Vaccine Delivery System
Current Drug Delivery Integrin αvβ3 as a Therapeutic Target for Blocking Tumor-Induced Angiogenesis
Current Drug Targets Current and Potential Anticancer Drugs Targeting Members of the UHRF1 Complex Including Epigenetic Modifiers
Recent Patents on Anti-Cancer Drug Discovery Patent Annotations
Recent Patents on Anti-Infective Drug Discovery Drug-Mediated Targeted Disruption of Multiple Protein Activities Through Functional Inhibition of the Hsp90 Chaperone Complex
Current Medicinal Chemistry Recent Advances in the Use of Metallic Nanoparticles with Antitumoral Action - Review
Current Medicinal Chemistry In Vitro Regulatory Effect of Epididymal Serpin CRES on Protease Activity of Proprotein Convertase PC4/PCSK4
Current Molecular Medicine