Background: Adenosine receptors (ARs) are classified as A1, A2A, A2B, and A3 subtypes belong to the superfamily of G-protein coupled receptors (GPCRs). More than 40% of modern medicines act through either activation or inhibition of signaling processes associated with GPCRs. In particular, A2B AR signaling pathways are implicated in asthma, inflammation, cancer, ischemic hyperfusion, diabetes mellitus, cardiovascular diseases, gastrointestinal disorders, and kidney disease.
Methods: This article reviews different disease segments wherein A2B AR is implicated and discusses the potential role of subtype-selective A2B AR ligands in the management of such diseases or disorders. All the relevant publications on this topic are reviewed and presented scientifically.
Results: This review provides an up-to-date highlight of the recent advances in the development of novel and selective A2B AR ligands and their therapeutic role in treating various disease conditions. A special focus has been given to the therapeutic potentials of selective A2B AR ligands in the management of airway inflammatory conditions and cancer.
Conclusions: This systematic review demonstrates the current status and perspectives of A2B AR ligands as therapeutically useful agents that would assist medicinal chemists and pharmacologists in discovering novel and subtype-selective A2B AR ligands as potential drug candidates.
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http://dx.doi.org/10.2174/1381612825666190717105834 | DOI Listing |
Mol Divers
January 2025
Chemometrics and Cheminformatics Laboratory, Department of Analytical Chemistry, Tarbiat Modares University, Tehran, Iran.
Adenosine receptors (A, A, A, A) play critical roles in cellular signaling and are implicated in various physiological and pathological processes, including inflammations and cancer. The main aim of this research was to investigate structure-activity relationships (SAR) to derive models that describe the selectivity and activity of inhibitors targeting Adenosine receptors. Structural information for 16,312 inhibitors was collected from BindingDB and analyzed using machine learning methods.
View Article and Find Full Text PDFChemistryOpen
November 2024
Departamento de Química Inorgánica, Universidad de Santiago de Compostela, E-, 15782, Santiago de Compostela, Spain.
Chemistry
January 2025
Research Center for Macromolecules and Biomaterials, National Institute for Materials Science: NIMS, 1-2-1 Sengen, Tsukuba, Ibaraki, 305-0032, Japan.
Supramolecular interactions between polymers play a crucial role in the construction of three-dimensional polymer structures with unique physical and chemical properties. In this study, we have fabricated a novel supramolecular miktoarm star copolymer (μ-star) with a cobalt(II) phthalocyanine (CoPc) core using metal-ligand coordination. Axial coordination of the terminal pyridyl group of poly(methyl methacrylate) with the CoPc core of four-armed star-shaped polystyrene provided AB- and AB-type μ-stars through stepwise complexation.
View Article and Find Full Text PDFHypertension
December 2024
Department of Pharmacology and Chemical Biology (E.K.J., S.P.T., Y.C., L.A.B.), University of Pittsburgh School of Medicine, Pittsburgh, PA.
Research in purinergic pharmacology has yielded major advances in cardiovascular therapeutics such as adenosine for terminating atrioventricular reentrant tachycardia, regadenoson for pharmacological ischemic stress testing, and selective P2Y receptor antagonists for prevention of stroke and myocardial infarction. Mechanistically, these FDA-approved purine-based therapeutics activate or antagonize receptors having endogenous ligands containing the purine nucleobase adenine. Recent discoveries suggest a novel direction for purine-based therapeutics.
View Article and Find Full Text PDFChem Asian J
January 2025
College of Science and Engineering, James Cook University,Townsville, Qld, 4811, Australia.
Reaction of lanthanoid tris(3,5-dimethylpyrazolate) compounds, [Ln(Mepz)(thf)] (Ln=La 1 a, Ce, Pr, Dy 1 b, Yb, Lu) with potassium or lithium bistrimethylsilylamide and with or without added 3,5-dimethylpyrazole, or of lanthanoid tris(bistrimethylsilyl)amide complexes with potassium bistrimethylsilylamide and 3,5-dimethylpyrazole have yielded a variety of oxide centred Ln or Ln/(K or Li) multinuclear cages, namely, [LaO(Mepz) K(thf)] (2 a), [LaO(Mepz)Li(MepzH)]⋅0.5Hexane (2 b), [LaO(Mepz)(MepzH)] (2 c) (from heating 1 a in toluene), [CeO(Mepz)K(dme)] (3 a), [CeO(Mepz)Li(thf)]⋅0.5Hexane (3 b) and [Ce(Mepz)Li(thf)] (3 c), which crystallized together, [CeO(Mepz)K(thf)] (3 d), [PrO(Mepz)K(thf)] (4), [DyO(Mepz)K(thf)]⋅THF (5), [YbO(Mepz)K(thf)]⋅THF (6), and [LuO(Mepz)K(thf)]⋅THF (7).
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