Abstract
The A3 adenosine receptors (A3 ARs), belonging to the adenosine receptor family of G-protein-coupled receptors (GPCRs), are ubiquitously expressed in a wide variety of tissues in human body, with high levels in peripheral organs and low levels in the brain. The A3 ARs are involved in a variety of important patho-physiological processes, including modulation of cerebral and cardiac ischemic damage, inflammation, modulation of intraocular pressure, regulation of normal and tumor cell growth, and immunosuppression. Consequently, A3 AR selective ligands may represent important pharmacological tools in the treatment of a variety of diseases. Indeed, the development of potent and selective A3 AR ligands has been the subject of medicinal chemistry research for more than two decades. Although to date a considerable number of selective A3 AR agonists and antagonists have been discovered, much is still to be learned about the exact function of this subtype, due to its enigmatic role in several physiological processes. In the last two decades, numerous medicinal chemistry groups have made intense efforts in searching for ideal ligands for the A3 AR subtype. The purpose of this review is to summarize the most recent developments made in the field of selective A3 AR ligands, which have been subdivided on the basis of their main chemical structural features. For each chemical class, attention has been focused on the SARs which determine ligand affinity and selectivity for the target subtype, and on eventually available preclinical data.
Keywords: Adenosine Receptor (AR), A3 AR ligands, structure-activity relationships, binding affinity, AR subtype selectivity
Current Topics in Medicinal Chemistry
Title: A3 Receptor Ligands: Past, Present and Future Trends
Volume: 10 Issue: 10
Author(s): S. Taliani, I. Pugliesi, M. Bellandi, C. La Motta and F. Da Settimo
Affiliation:
Keywords: Adenosine Receptor (AR), A3 AR ligands, structure-activity relationships, binding affinity, AR subtype selectivity
Abstract: The A3 adenosine receptors (A3 ARs), belonging to the adenosine receptor family of G-protein-coupled receptors (GPCRs), are ubiquitously expressed in a wide variety of tissues in human body, with high levels in peripheral organs and low levels in the brain. The A3 ARs are involved in a variety of important patho-physiological processes, including modulation of cerebral and cardiac ischemic damage, inflammation, modulation of intraocular pressure, regulation of normal and tumor cell growth, and immunosuppression. Consequently, A3 AR selective ligands may represent important pharmacological tools in the treatment of a variety of diseases. Indeed, the development of potent and selective A3 AR ligands has been the subject of medicinal chemistry research for more than two decades. Although to date a considerable number of selective A3 AR agonists and antagonists have been discovered, much is still to be learned about the exact function of this subtype, due to its enigmatic role in several physiological processes. In the last two decades, numerous medicinal chemistry groups have made intense efforts in searching for ideal ligands for the A3 AR subtype. The purpose of this review is to summarize the most recent developments made in the field of selective A3 AR ligands, which have been subdivided on the basis of their main chemical structural features. For each chemical class, attention has been focused on the SARs which determine ligand affinity and selectivity for the target subtype, and on eventually available preclinical data.
Export Options
About this article
Cite this article as:
Taliani S., Pugliesi I., Bellandi M., La Motta C. and Da Settimo F., A3 Receptor Ligands: Past, Present and Future Trends, Current Topics in Medicinal Chemistry 2010; 10 (10) . https://dx.doi.org/10.2174/156802610791293109
DOI https://dx.doi.org/10.2174/156802610791293109 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
AlphaFold in Medicinal Chemistry: Opportunities and Challenges
AlphaFold, a groundbreaking AI tool for protein structure prediction, is revolutionizing drug discovery. Its near-atomic accuracy unlocks new avenues for designing targeted drugs and performing efficient virtual screening. However, AlphaFold's static predictions lack the dynamic nature of proteins, crucial for understanding drug action. This is especially true for multi-domain proteins, ...read more
Artificial intelligence for Natural Products Discovery and Development
Our approach involves using computational methods to predict the potential therapeutic benefits of natural products by considering factors such as drug structure, targets, and interactions. We also employ multitarget analysis to understand the role of drug targets in disease pathways. We advocate for the use of artificial intelligence in predicting ...read more
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...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
- Announcements
Related Articles
-
Strategies for Leukotriene Modulation in Dermatology: Even More Visionary Perspectives? An Update
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Vitamin D and Stroke: Promise for Prevention and Better Outcome
Current Vascular Pharmacology Wip1-Deficient Neutrophils Significantly Promote Intestinal Ischemia/Reperfusion Injury in Mice
Current Molecular Medicine Vitamin D Therapy in Cardiac Hypertrophy and Heart Failure
Current Pharmaceutical Design Salvia miltiorrhiza: A Potential Red Light to the Development of Cardiovascular Diseases
Current Pharmaceutical Design Mediterranean Diet and Dementia of the Alzheimer Type
Current Aging Science Human Chorionic Gonadotropin: A Model Molecule For Oligopeptide-Based Drug Discovery
Endocrine, Metabolic & Immune Disorders - Drug Targets Antioxidant Properties and Associated Mechanisms of Salicylates
Current Medicinal Chemistry Coronary Artery Disease in Patients with Chronic Kidney Disease: A Clinical Update
Current Cardiology Reviews The Janus Face of Cathelicidin in Tumorigenesis
Current Medicinal Chemistry Lipid-Lowering Therapies for Atherosclerosis: Statins, Fibrates, Ezetimibe and PCSK9 Monoclonal Antibodies
Current Medicinal Chemistry Contrasting Roles of the Galectin-3 in the Schizophrenia Onset, Clinical Presentation, and Somatic Comorbidity
Current Topics in Medicinal Chemistry High Mobility Group Box 1 Protein as a Potential Drug Target for Infection- and Injury-Elicited Inflammation
Inflammation & Allergy - Drug Targets (Discontinued) Assessment of Cardiac Sympathetic Innervation in Heart Failure and Lethal Arrhythmias: Therapeutic and Prognostic Implications
Current Cardiology Reviews Novel Drug Targets for the Treatment of Cardiac Diseases
Current Pharmacogenomics and Personalized Medicine Insights in microRNAs Biology
Current Topics in Medicinal Chemistry In the Search of the Vulnerable Plaque: Current Diagnostic Techniques and Future Directions
Vascular Disease Prevention (Discontinued) COXIBs, CINODs and H2S-Releasing NSAIDs: Current Perspectives in the Development of Safer Non Steroidal Anti-Inflammatory Drugs
Current Medicinal Chemistry Microvascular (dys)Function in Stable Coronary Artery Disease: Cross Talk with Epicardial Segments
Current Pharmaceutical Design Therapeutic Impact of Sphingosine 1-phosphate Receptor Signaling in Multiple Sclerosis
Mini-Reviews in Medicinal Chemistry