Abstract
Oligosaccharide processing enzymes such as glycosidases and glycosyltransferases are important classes of biocatalysts involved in synthesising specific oligosaccharide structures on proteins and lipids. These enzymes are known to be involved in a wide range of important biological processes, such as intestinal digestion, post-translational processing of glycoproteins, lysosomal catabolism of glycoconjugates and inter-cellular recognition events. Inhibition of these enzymes can disrupt biosynthesis of oligosaccharides, thus interfering in all of these processes. Hence, “glyco-enzyme” inhibitors might have enormous therapeutic potential in many diseases such as viral infection, cancer and diabetes. This very important prospect has led to increasing interest and demand for these compounds. Interference in oligosaccharide processing is the basis for the anti-influenza neuraminidase inhibitors that have recently been marketed and also for the potential use of glycosidase inhibitors against HIV, Gauchers disease, hepatitis, and cancer. Since a rational design and synthesis of inhibitors are often extremely difficult due to the limited information regarding the structure of the active site, combinatorial approaches are particularly promising. This review will focus on synthetic efforts for the preparation of combinatorial libraries of glyco-enzyme inhibitors.
Keywords: iminosugar libraries, enzyme inhibitors, glycosyltransferases, glycosidases, carbohydrate analogues, Iminosugars
Combinatorial Chemistry & High Throughput Screening
Title: Combinatorial Approaches to Iminosugars as Glycosidase and Glycosyltransferase Inhibitors
Volume: 9 Issue: 8
Author(s): Maria Gregori, Barbara La Ferla and Laura Cipolla
Affiliation:
Keywords: iminosugar libraries, enzyme inhibitors, glycosyltransferases, glycosidases, carbohydrate analogues, Iminosugars
Abstract: Oligosaccharide processing enzymes such as glycosidases and glycosyltransferases are important classes of biocatalysts involved in synthesising specific oligosaccharide structures on proteins and lipids. These enzymes are known to be involved in a wide range of important biological processes, such as intestinal digestion, post-translational processing of glycoproteins, lysosomal catabolism of glycoconjugates and inter-cellular recognition events. Inhibition of these enzymes can disrupt biosynthesis of oligosaccharides, thus interfering in all of these processes. Hence, “glyco-enzyme” inhibitors might have enormous therapeutic potential in many diseases such as viral infection, cancer and diabetes. This very important prospect has led to increasing interest and demand for these compounds. Interference in oligosaccharide processing is the basis for the anti-influenza neuraminidase inhibitors that have recently been marketed and also for the potential use of glycosidase inhibitors against HIV, Gauchers disease, hepatitis, and cancer. Since a rational design and synthesis of inhibitors are often extremely difficult due to the limited information regarding the structure of the active site, combinatorial approaches are particularly promising. This review will focus on synthetic efforts for the preparation of combinatorial libraries of glyco-enzyme inhibitors.
Export Options
About this article
Cite this article as:
Gregori Maria, La Ferla Barbara and Cipolla Laura, Combinatorial Approaches to Iminosugars as Glycosidase and Glycosyltransferase Inhibitors, Combinatorial Chemistry & High Throughput Screening 2006; 9 (8) . https://dx.doi.org/10.2174/138620706778249703
DOI https://dx.doi.org/10.2174/138620706778249703 |
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
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...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
- 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
-
Mutations of mtDNA in some Vascular and Metabolic Diseases
Current Pharmaceutical Design Diabetes, Cognitive Function, and the Blood-Brain Barrier
Current Pharmaceutical Design Dabigatran Reversal with Idarucizumab in an Emergency Lumbar Puncture: A Case Report
Current Drug Safety Structural Heterogeneity and Multifunctionality of Lactoferrin
Current Protein & Peptide Science Genomic Databases and the Search of Protein Targets for Protozoan Parasites
Current Drug Targets SRLVs: A Genetic Continuum of Lentiviral Species in Sheep and Goats with Cumulative Evidence of Cross Species Transmission
Current HIV Research From Surface to Nuclear Receptors: The Endocannabinoid Family Extends its Assets
Current Medicinal Chemistry Curcumin: Structure-Activity Relationship Towards its Role as a Versatile Multi-Targeted Therapeutics
Mini-Reviews in Organic Chemistry Vaccine-Associated Neurological Adverse Events: A Case Report and Literature Review
Current Pharmaceutical Design Delivery of Anti-Viral Nucleoside Analogues to the Central Nervous System
Current Medicinal Chemistry - Anti-Infective Agents Directing the Antiretroviral Drugs to the Brain Reservoir: A Nanoformulation Approach for NeuroAIDS
Current Drug Metabolism Chemotherapy In Japanese Encephalitis: Are We There Yet?
Infectious Disorders - Drug Targets Human Parvovirus B19: An Infectious Agent with the Potential to Induce and Trigger Rheumatic Disease
Current Rheumatology Reviews Cellular Reservoirs of HIV-1 and their Role in Viral Persistence
Current HIV Research Regulation of Apoptosis by Gram-Positive Bacteria: Mechanistic Diversity and Consequences for Immunity
Current Immunology Reviews (Discontinued) Autoimmune Diseases and Atherosclerosis: The Inflammatory Connection
Current Immunology Reviews (Discontinued) Base Distribution in Dengue Nucleotide Sequences Differs Significantly from Other Mosquito-Borne Human-Infecting Flavivirus Members
Current Computer-Aided Drug Design Potential Factors Induced by Filoviruses that Lead to Immune Supression
Current Molecular Medicine Gene Therapy and Biologic Therapy with Interleukin?4
Current Gene Therapy Molecular Mechanisms Involved in the Aging of the T-cell Immune Response
Current Genomics