G protein–coupled receptors (GPCRs) constitute the largest family of membrane proteins in
the human genome and are important therapeutic targets. During the last decade, the …

In recent years, several novel aspects of GPCR pharmacology have been described, which
are thought to play a role in determining the in vivo efficacy of a compound. Fluorescent …

Rational drug design for G protein-coupled receptors (GPCRs) is limited by the small
number of available atomic resolution structures. We assessed the use of homology …

The growing number of studies on G protein-coupled receptors (GPCRs) family are a source
of noticeable improvement in our understanding of the functioning of these proteins. GPCRs …

G protein-coupled receptors (GPCRs) make up the largest receptor superfamily, accounting
for 4% of protein-coding genes. Despite the prevalence of such transmembrane receptors, a …

In silico methods like molecular docking and pharmacophore modeling are established
strategies in lead identification. Their successful application for finding new active molecules …

The determination of G protein-coupled receptor (GPCR) structures at atomic resolution has
improved understanding of cellular signaling and will accelerate the development of new …

Fragment-based drug discovery (FBDD) is now well-established as a technology for
generating new chemical leads and drugs. This Miniperspective provides a tabulated …

Highlights•Antagonists of A 2B adenosine receptor (A 2B AR) have potential for the
treatment of asthma and COPD.•Computer aided drug design (CADD) strategies used in the …

Fragment-based lead discovery has emerged as a leading drug development strategy for
novel therapeutic targets. Although fragment-based drug discovery benefits immensely from …