Abstract
Over the past 15 years the privileged structure concept has emerged as a fruitful approach to the discovery of novel biologically active molecules. Privileged structures are molecular scaffolds with versatile binding properties, such that a single scaffold is able to provide potent and selective ligands for a range of different biological targets through modification of functional groups. In addition, privileged structures typically exhibit good drug-like properties, which in turn leads to more drug-like compound libraries and leads. The net result is the production of high quality leads that provide a solid foundation for further development. The identification of privileged structures will be discussed, emphasizing the importance of understanding the structure-target relationships that confer “privileged” status. This understanding allows privileged structure based libraries to be targeted at distinct target families (e.g. GPCRs, LGIC, enzymes / kinases). Privileged structures have been successfully exploited across and within different target families and promises to be an effective approach to the discovery and optimization of novel bioactive molecules. The application of the privileged structure approach, both in traditional medicinal chemistry and in the design of focused libraries, will be discussed with the aid of illustrative examples.
Keywords: privileged structures, drug like properties, combinatorial libraries, focused libraries
Combinatorial Chemistry & High Throughput Screening
Title: Privileged Structures: Applications in Drug Discovery
Volume: 7 Issue: 5
Author(s): R. W. DeSimone, K. S. Currie, S. A. Mitchell, J. W. Darrow and D. A. Pippin
Affiliation:
Keywords: privileged structures, drug like properties, combinatorial libraries, focused libraries
Abstract: Over the past 15 years the privileged structure concept has emerged as a fruitful approach to the discovery of novel biologically active molecules. Privileged structures are molecular scaffolds with versatile binding properties, such that a single scaffold is able to provide potent and selective ligands for a range of different biological targets through modification of functional groups. In addition, privileged structures typically exhibit good drug-like properties, which in turn leads to more drug-like compound libraries and leads. The net result is the production of high quality leads that provide a solid foundation for further development. The identification of privileged structures will be discussed, emphasizing the importance of understanding the structure-target relationships that confer “privileged” status. This understanding allows privileged structure based libraries to be targeted at distinct target families (e.g. GPCRs, LGIC, enzymes / kinases). Privileged structures have been successfully exploited across and within different target families and promises to be an effective approach to the discovery and optimization of novel bioactive molecules. The application of the privileged structure approach, both in traditional medicinal chemistry and in the design of focused libraries, will be discussed with the aid of illustrative examples.
Export Options
About this article
Cite this article as:
DeSimone W. R., Currie S. K., Mitchell A. S., Darrow W. J. and Pippin A. D., Privileged Structures: Applications in Drug Discovery, Combinatorial Chemistry & High Throughput Screening 2004; 7 (5) . https://dx.doi.org/10.2174/1386207043328544
DOI https://dx.doi.org/10.2174/1386207043328544 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...read more
Integrating Network Pharmacology and Traditional Medicine: A New Perspective in Drug Mechanism Research
Network pharmacology is a network construction and network topology analysis strategy that combines pharmacology and pharmacodynamics. In recent years, network pharmacology has emerged as a powerful tool that can be integrated with pharmacology. Natural products commonly function in multicomponent, multitarget, and multipathway systems. Some examples encompass Ayurveda, traditional Chinese medicines ...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
Related Articles
-
The GH/IGF-1 Axis in Chronic Heart Failure
Endocrine, Metabolic & Immune Disorders - Drug Targets The Emerging Role of Metabotropic Glutamate Receptors in the Pathophysiology of Chronic Stress-Related Disorders
Current Neuropharmacology Current and Future Applications of Probiotics
Current Nutrition & Food Science Fibroblast Growth Factors, Fibroblast Growth Factor Receptors, Diseases, and Drugs
Recent Patents on Cardiovascular Drug Discovery Approaches Targeting KV10.1 Open a Novel Window for Cancer Diagnosis and Therapy
Current Medicinal Chemistry Pediatric Health Effects of Chronic Exposure to Extremely Low Frequency Electromagnetic Fields
Current Pediatric Reviews Herbal and Traditional Chinese Medicine for the Treatment of Cardiovascular Complications in Diabetes Mellitus
Current Diabetes Reviews The Proteolytic Activation of Angiogenic and Lymphangiogenic Growth Factors in Cancer – Its Potential Relevance for Therapeutics and Diagnostics
Current Medicinal Chemistry Proteasome Structure, Function, and Lessons Learned from Beta-Lactone Inhibitors
Current Topics in Medicinal Chemistry Prostate Cancer Horizons in the Development of Novel Anti-Cancer Strategies
Current Medicinal Chemistry - Anti-Cancer Agents The IGF Axis in Prostate Cancer
Current Pharmaceutical Design Relationships between Serotoninergic System and Skin Fibrotic
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Mitochondria, Cellular Stress Resistance, Somatic Cell Depletion and Lifespan
Current Aging Science Genetics of the First Seven Proprotein Convertase Enzymes in Health and Disease
Current Genomics Diagnostic and Therapeutic Use of Human Recombinant Thyrotropin (rhTSH)(Thyrogen®) in Well-Differentiated Thyroid Cancer - Current Indications and Future Perspectives - A Review
Current Pharmaceutical Analysis Green Tea (Camellia sinensis) Protects Against Arsenic Neurotoxicity via Antioxidative Mechanism and Activation of Superoxide Dismutase Activity
Central Nervous System Agents in Medicinal Chemistry The Effects of Weightlessness on the Human Organism and Mammalian Cells
Current Molecular Medicine MicroRNA-21: From Cancer to Cardiovascular Disease
Current Drug Targets Recent Advances in GNAS Epigenetic Research of Pseudohypoparathyroidism
Current Molecular Medicine Leukotriene A4 Hydrolase as a Target for Cancer Prevention and Therapy
Current Cancer Drug Targets