In the search for new therapeutic agents for currently incurable diseases, attention has
turned to traditionally “undruggable” targets, and collections of drug-like small molecules …

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 …

G protein-coupled receptors (GPCRs) comprise the largest family of transmembrane
proteins. For GPCR drug discovery, it is important that ligand affinity is determined in the …

The discovery of bioactive compounds underpins many areas of basic biomedical research
and constitutes a large part of medicinal chemistry and chemical biology. Synthetic …

Conspectus Protein–protein interactions (PPIs) are essential in numerous biological
processes and diseases, making them attractive yet challenging drug targets. While many …

Three novel families of A2B adenosine receptor antagonists were identified in the context of
the structural exploration of the 3, 4-dihydropyrimidin-2 (1 H)-one chemotype. The most …

We describe the discovery and optimization of 3, 4-dihydropyrimidin-2 (1 H)-ones as a novel
family of (nonxanthine) A2B receptor antagonists that exhibit an unusually high selectivity …

Diversity-oriented synthesis (DOS) can provide a collection of diverse and complex drug-like
small molecules, which is critical in the development of new chemical probes for biological …

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 …

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 …