The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in

However, the etiology and pathogenesis of preeclampsia are complicated and have not been fully elucidated

Mrgpra2 were critical for combating S. aureus infections and the formation of neutrophil abscesses, a hallmark

treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR have The results demonstrate that virtual screens of fragment- and lead-like chemical libraries have complementary

Recordings in brain slices have shown that co-activation using saturating concentrations of agonists

Mouse models have provided invaluable information on the roles for PKA subunits in brain and key metabolic

The physiological activities of UCPs have been hotly contested, and the involvement of UCPs in the pathogenesis

Recently, academic and industrial scientific communities involved in kinetics-based drug development have Here, we have implemented an optimized approach of combining the data derived from steered molecular We have predicted the absolute ligand residence times on the timescale of seconds.

Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new In less than a decade, nanobodies, or recombinant single-domain antibody fragments from camelids, have Nanobodies have gained traction rapidly due to their biochemical tractability and their ability to recognize Here, we review how nanobodies have been adopted to elucidate the structure, pharmacology, and signaling

However, the available tools to dissect the endogenous dopaminergic circuits have limited specificity

selectivity and allosteric modulation in angiotensin receptors: IUPHAR Review 34 "Functional advances have structures of both AngII receptors (AT1 and AT2 receptors) bound to peptide and non-peptide ligands have

Recent advances in X-ray crystallography and cryo-EM have resulted in a wealth of GPCR structures that have been used in drug design and formed the basis for mechanistic activation hypotheses.

While traditional drug discovery programs have focused on the development of ligands targeting the binding advances in the structure determination of GPCRs bound to different types of allosteric modulators have

target in colorectal cancer using novel fluorescent GPCR ligands "G-protein coupled receptors (GPCRs) have been largely targeted in a wide range of diseases, but few therapies have been directed against GPCRs

Intriguingly, the two ligands have distinct signaling and physiological properties: PTH evokes prolonged

We summarize recent discoveries that have advanced our understanding of rod outer segment (ROS) morphology We have combined recently published cryo-electron tomography (cryo-ET) data on the ROS with structural

for the A2A Adenosine Receptor "Modulators of the G protein-coupled A2A adenosine receptor (A2AAR) have

Furthermore, a plethora of TRPM3 variants that result from alternative splicing have been identified Therefore, the newest data related to TRPM3 have to be discussed and to be put in context as soon as

The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in

which members of the G protein-coupled receptor (GPCR) family respond to neurotransmitters in the brain have

partners available today do not reveal a clear conformational basis for signaling bias, which would have

In the current study, we have further characterized this H3R biosensor on intact cells by monitoring In addition, we have validated the H3R biosensor in membrane preparations and found that observed potency

protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have The structure, function, and involvement of adhesion GPCRs in cancer development have been discussed

However, GRKs have not been directly implicated in regulation of the amyloid-β (Aβ) pathogenic cascade

We have previously shown interaction between PKR2 and anosmin 1 in vitro.

A variety of ligands for CB1 receptors have been developed as promising drug candidates for the treatment New high-resolution structures of CB1 receptor in different functional states have significantly improved These advances have paved the way for development of novel ligands for different therapeutic applications

Although studies have focused on the G-protein signaling state, the mechanism for β-arrestin signaling Studies have indicated that transmembrane helix 7 (TMH7) and the highly conserved NPXXY motif can be

On the other hand, they showed the ability to couple with Gαq/11 protein and make Ca2+ mobilization at