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
-
Recent Aspects of Osmotic Pump Systems: Functionalization, Clinical use and Advanced Imaging Technology
Current Drug Metabolism Recent Advancements in Fuzzy C-means Based Techniques for Brain MRI Segmentation
Current Medical Imaging New Cathepsin D Inhibitorswith Hydroxyethylamine Isosteres: Preparation and Characterization
Medicinal Chemistry Nitric Oxide and Teratogenesis: An Update
Current Pharmaceutical Design BOOK REVIEW : New Frontiers in Mirror Neurons Research
Current Aging Science The Use of Chronobiotics in the Resynchronization of the Sleep/Wake Cycle. Therapeutical Application in the Early Phases of Alzheimer's Disease
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery Gene Therapy for Neuroprotection and Neurorestoration (Part I)
Current Gene Therapy Hydrogen Sulphide and Pain
Inflammation & Allergy - Drug Targets (Discontinued) Identification of Potent Caspase-3 Inhibitors for Treatment of Multi- Neurodegenerative Diseases Using Pharmacophore Modeling and Docking Approaches
CNS & Neurological Disorders - Drug Targets Structure-Activity Relationships in Peptide-Antibody Complexes: Implications for Epitope Prediction and Development of Synthetic Peptide Vaccines
Current Medicinal Chemistry The CCL2/CCR2 Axis in the Pathogenesis of HIV-1 Infection: A New Cellular Target for Therapy?
Current Drug Targets Intercalation of Erlotinib and Pemetrexed in the Treatment of Non-Small Cell Lung Cancer
Current Drug Targets Novel Approaches to the Pharmacotherapy of Obesity
Current Pharmaceutical Design Histamine H3 Receptor: A Potential Drug Target for the Treatment of Central Nervous System Disorders
Current Drug Targets - CNS & Neurological Disorders The Role of FKBP5 in Mood Disorders: Action of FKBP5 on Steroid Hormone Receptors Leads to Questions About its Evolutionary Importance
CNS & Neurological Disorders - Drug Targets Should Adolescents be Screened for Depression?
Adolescent Psychiatry Disturbed Sleep Patterns in Elders with Mild Cognitive Impairment: The Role of Memory Decline and ApoE ε 4 Genotype
Current Alzheimer Research Molecular Modelling Studies on Thiazole-Based α-Glucosidase Inhibitors Using Docking and CoMFA, CoMSIA and HQSAR
Current Drug Discovery Technologies ADAM17 as a Therapeutic Target in Multiple Diseases
Current Pharmaceutical Design Mechanisms of the Blunting of the Sympatho-Adrenal Response: A Theory
Current Diabetes Reviews