Medicinal chemical approaches have been applied to all four of the adenosine receptor
(AR) subtypes (A1, A2A, A2B, and A3) to create selective agonists and antagonists for each …

The A3 adenosine receptor (A3AR) subtype is a novel, promising therapeutic target for
inflammatory diseases, such as rheumatoid arthritis (RA) and psoriasis, as well as liver …

In 1998, Bikker, Trumpp-Kallmeyer, and Humblet published a Perspective in this journal
entitled “G-Protein Coupled Receptors: Models, Mutagenesis and Drug Design” and …

The trend toward designing large hydrophobic molecules for lead optimization is often
associated with poor drug-likeness and high attrition rates in drug discovery and …

G protein‐coupled receptors (GPCRs) are an important family of membrane proteins;
historically, drug discovery in this target class has been fruitful, with many of the world's top …

Any aspect of cell activity is regulated by extracellular signals that are recognized, decoded,
and transduced inside the cell via different classes of plasma membrane receptors. 1À3 G …

Our understanding of the structural biology of G protein-coupled receptors has undergone a
transformation over the past 5 years. New protein–ligand complexes are described almost …

Abstract Pyrazolo [4, 3-d] pyrimidine, a fused heterocycle bearing pyrazole and pyrimidine
portions has gained a significant attention in the field of bioorganic and medicinal chemistry …

Two regioisomeric series of diaryl 2-or 4-amidopyrimidines have been synthesized and their
adenosine receptor affinities were determined in radioligand binding assays at the four …

The crystal structure of the human A2A adenosine receptor, a member of the G protein-
coupled receptor (GPCR) family, is used as a starting point for the structural characterization …