Abstract
Alzheimer’s disease (AD), a degenerative disease affecting the brain, is the single most common source of dementia in adults. The cause and the progression of AD still remains a mystery among medical experts. As a result, a cure has not yet been discovered, even after decade’s worth of research that started since 1906, when the disease was first identified. Despite the efforts of the scientific community, several of the biological receptors associated with AD have not been sufficiently studied to date, limiting in turn the design of new and more potent anti-AD agents. Thus, the search for new drug candidates as inhibitors of different targets associated with AD constitutes an essential part towards the discovery of new and more efficient anti-AD therapies. The present work is focused on the role of the Ligand-Based Drug Design (LBDD) methodologies which have been applied for the elucidation of new molecular entities with high inhibitory activity against targets related with AD. Particular emphasis is given also to the current state of fragment-based ligand approaches as alternatives of the Fragment-Based Drug Discovery (FBDD) methodologies. Finally, several guidelines are offered to show how the use of fragment-based descriptors can be determinant for the design of multi-target inhibitors of proteins associated with AD.
Keywords: Alzheimer’s Disease (AD), Anti-AD Agents, Amyloid β -A4 Protein, Fragment-Based Drug Discovery, Glycogen Synthase Kinase-3β, Ligand-Based Drug Design, Linear Discriminant Analysis, Monoamine Oxidase B, Multi-Target Inhibitors, QSAR, Quantitative Contributions
Current Medicinal Chemistry
Title:Role of Ligand-Based Drug Design Methodologies toward the Discovery of New Anti- Alzheimer Agents: Futures Perspectives in Fragment-Based Ligand Design
Volume: 19 Issue: 11
Author(s): A. Speck-Planche, F. Luan and M. N.D.S. Cordeiro
Affiliation:
Keywords: Alzheimer’s Disease (AD), Anti-AD Agents, Amyloid β -A4 Protein, Fragment-Based Drug Discovery, Glycogen Synthase Kinase-3β, Ligand-Based Drug Design, Linear Discriminant Analysis, Monoamine Oxidase B, Multi-Target Inhibitors, QSAR, Quantitative Contributions
Abstract: Alzheimer’s disease (AD), a degenerative disease affecting the brain, is the single most common source of dementia in adults. The cause and the progression of AD still remains a mystery among medical experts. As a result, a cure has not yet been discovered, even after decade’s worth of research that started since 1906, when the disease was first identified. Despite the efforts of the scientific community, several of the biological receptors associated with AD have not been sufficiently studied to date, limiting in turn the design of new and more potent anti-AD agents. Thus, the search for new drug candidates as inhibitors of different targets associated with AD constitutes an essential part towards the discovery of new and more efficient anti-AD therapies. The present work is focused on the role of the Ligand-Based Drug Design (LBDD) methodologies which have been applied for the elucidation of new molecular entities with high inhibitory activity against targets related with AD. Particular emphasis is given also to the current state of fragment-based ligand approaches as alternatives of the Fragment-Based Drug Discovery (FBDD) methodologies. Finally, several guidelines are offered to show how the use of fragment-based descriptors can be determinant for the design of multi-target inhibitors of proteins associated with AD.
Export Options
About this article
Cite this article as:
Speck-Planche A., Luan F. and N.D.S. Cordeiro M., Role of Ligand-Based Drug Design Methodologies toward the Discovery of New Anti- Alzheimer Agents: Futures Perspectives in Fragment-Based Ligand Design, Current Medicinal Chemistry 2012; 19 (11) . https://dx.doi.org/10.2174/092986712799945058
DOI https://dx.doi.org/10.2174/092986712799945058 |
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
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
Current advances in inherited cardiomyopathy
Describe in detail all novel advances in multimodality imaging related to inherited cardiomyopathy diagnosis and prognosis. Shed light to deeper phenotypic characterization. Acknowledge recent advances in genetics, genomics and precision medicineread 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
-
In Vitro Blood-Brain Barrier Models – Latest Advances and Therapeutic Applications in a Chronological Perspective
Mini-Reviews in Medicinal Chemistry Heat Shock Proteins And Neuroprotection
Recent Patents on DNA & Gene Sequences Novel Multifunctional Anti-Alzheimer Drugs with Various CNS Neurotransmitter Targets and Neuroprotective Moieties
Current Alzheimer Research Melatonin Therapy of Pediatric Sleep Disorders: Recent Advances, Why it Works, Who are the Candidates and How to Treat
Current Pediatric Reviews Incidence and Prevalence of Hypothyroidism in Patients Affected by Chronic Heart Failure: Role of Amiodarone
Endocrine, Metabolic & Immune Disorders - Drug Targets Interactions Between Apo E and Amyloid Beta and their Relationship to Nutriproteomics and Neurodegeneration
Current Proteomics Cellular Mechanisms of the Protective Effect of Polyphenols on the Neurovascular Unit in Strokes
Cardiovascular & Hematological Agents in Medicinal Chemistry Antioxidants in the Treatment of Diabetes
Current Diabetes Reviews Alterations in Homocysteine Metabolism Among Alcohol Dependent Patients - Clinical, Pathobiochemical and Genetic Aspects
Current Drug Abuse Reviews Targeting Oxidative Stress Component in the Therapeutics of Epilepsy
Current Topics in Medicinal Chemistry Patent Selections
Recent Patents on CNS Drug Discovery (Discontinued) New Approaches in Nuclear Medicine for Early Diagnosis of Alzheimers Disease
Current Alzheimer Research Cannabidiol and Sodium Nitroprusside: Two Novel Neuromodulatory Pharmacological Interventions to Treat and Prevent Psychosis
CNS & Neurological Disorders - Drug Targets Neuroprotective Effects of Drug-Induced Therapeutic Hypothermia in Central Nervous System Diseases
Current Drug Targets Polypeptide Models to Understand Misfolding and Amyloidogenesis and Their Relevance in Protein Design and Therapeutics
Protein & Peptide Letters Conference Report: The Myriad Pathways of Neurodegeneration Discussed at NEUROCON 2015
Current Aging Science Is Alpha-Synuclein Pathology a Target for Treatment of Neurodegenerative Disorders?
Current Alzheimer Research Quantitative μPET Imaging of Cerebral Glucose Metabolism and Amyloidosis in the TASTPM Double Transgenic Mouse Model of Alzheimer’s Disease
Current Alzheimer Research Evaluating Protein-protein Interaction (PPI) Networks for Diseases Pathway, Target Discovery, and Drug-design Using `In silico Pharmacology`
Current Protein & Peptide Science Decoding Common Features of Neurodegenerative Disorders: From Differentially Expressed Genes to Pathways
Current Genomics