Abstract
The Adenosine A2A receptor is a member of the G-protein coupled receptor superfamily. It plays a key role in numerous physiological processes through the central nervous system and in peripheral tissues. Functional interactions between the A2A and dopamine D2 receptor has spurred interest in the use of antagonists as anti-Parkinson drugs. Additionally, oncology drugs are now being designed based on the potential for A2A antagonists to function as immunotherapeutics. From early studies based on classical xanthine type A2A antagonists through second generation agents, this mini review will cover aspects of the discovery, development, chemical synthesis and medicinal evaluation of this important class of drugs.
Keywords: A2AR antagonists, aqueous solubility, cancer immunotherapy, molecular modeling, parkinson's disease, PET imaging, X-ray crystallography.
Current Medicinal Chemistry
Title:Towards Next Generation Adenosine A2A Receptor Antagonists
Volume: 21 Issue: 34
Author(s): G. Yuan and G.B. Jones
Affiliation:
Keywords: A2AR antagonists, aqueous solubility, cancer immunotherapy, molecular modeling, parkinson's disease, PET imaging, X-ray crystallography.
Abstract: The Adenosine A2A receptor is a member of the G-protein coupled receptor superfamily. It plays a key role in numerous physiological processes through the central nervous system and in peripheral tissues. Functional interactions between the A2A and dopamine D2 receptor has spurred interest in the use of antagonists as anti-Parkinson drugs. Additionally, oncology drugs are now being designed based on the potential for A2A antagonists to function as immunotherapeutics. From early studies based on classical xanthine type A2A antagonists through second generation agents, this mini review will cover aspects of the discovery, development, chemical synthesis and medicinal evaluation of this important class of drugs.
Export Options
About this article
Cite this article as:
Yuan G. and Jones G.B., Towards Next Generation Adenosine A2A Receptor Antagonists, Current Medicinal Chemistry 2014; 21 (34) . https://dx.doi.org/10.2174/0929867321666140826115123
DOI https://dx.doi.org/10.2174/0929867321666140826115123 |
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
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...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
- 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
-
Clinical Implications of CYP2D6 Genetic Polymorphism During Treatment with Antipsychotic Drugs
Current Drug Targets Advanced Magnetic Resonance Imaging Techniques in the Preterm Brain: Methods and Applications
Current Pediatric Reviews Omega-3 Polyunsaturated Fatty Acids in Alzheimers Disease: Key Questions and Partial Answers
Current Alzheimer Research Synthesis of Mannich Bases by Two Different Methods and Evaluation of their Acetylcholine Esterase and Carbonic Anhydrase Inhibitory Activities
Letters in Drug Design & Discovery An Inflammation-related Nutrient Pattern is Associated with Both Brain and Cognitive Measures in a Multiethnic Elderly Population
Current Alzheimer Research Systematic Review of Food Addiction as Measured with the Yale Food Addiction Scale: Implications for the Food Addiction Construct
Current Neuropharmacology Antitumor Potential and Possible Targets of Phenothiazine-Related Compounds
Current Drug Targets Intranasal Drug Delivery for Brain Targeting
Current Drug Delivery Anti-Depressant
Current Bioactive Compounds Regulation of the Urokinase Receptor (uPAR) by LDL Receptor-related Protein-1 (LRP1)
Current Pharmaceutical Design Neuro-psychopharmacogenetics and Neurological Antecedents of Posttraumatic Stress Disorder: Unlocking the Mysteries of Resilience and Vulnerability
Current Neuropharmacology Cardiovascular and Renovascular Implications of COX-2 Inhibition
Current Pharmaceutical Design Familial Alzheimers Disease Mutations in Presenilin 1 Do Not Alter Levels of the Secreted Amyloid-β Protein Precursor Generated by β-Secretase Cleavage
Current Alzheimer Research Characterization of the Non-Fibrillar α-Synuclein Oligomers
Protein & Peptide Letters Editorial (Thematic Issue: Future Trends in the Development of New Antidepressant Drugs)
Current Pharmaceutical Design Synaptic Aging is Associated with Mitochondrial Dysfunction, Reduced Antioxidant Contents and Increased Vulnerability to Amyloid-β Toxicity
Current Alzheimer Research Alterations in Homocysteine Metabolism Among Alcohol Dependent Patients - Clinical, Pathobiochemical and Genetic Aspects
Current Drug Abuse Reviews Efficacy of Sofosbuvir Plus Ribavirin with or Without Peginterferon- Alfa in Treatment of a Cohort of Egyptian Patients with Hepatitis C Virus Infection
Infectious Disorders - Drug Targets Neurotrophins - From Pathophysiology to Treatment in Alzheimers Disease
Current Alzheimer Research Substituted Urea Derivatives: A Potent Class of Antidepressant Agents
Medicinal Chemistry