Discovery of the First Potent and Orally Efficacious Agonist of the Orphan G-Protein Coupled Receptor 119 Graeme Semple *† , Beatriz Fioravanti † , Guillherme Pereira † , Imelda Calderon † , Jane Uy † ...

In both cases, the receptor was studied in complex with endogenous mammalian GnRH and the Gq protein. The researchers determined cryo-EM structures for the frog and pig GnRHR–Gq complexes at ...

However, efforts to determine the receptor’s structure have been hampered for decades by its low expression levels and inherent instability, leaving unresolved questions about how GnRH activates ...

The key compound (3f) is an arylazopyrazole-based antagonist targeting a prototypic family A G protein-coupled receptor (GPCR), the histamine H 3 receptor (H 3 R), and enabled convenient radiolabeling ...

Recent findings on spatial organization of G-protein coupled receptors provide additional support for this framework, demonstrating that the coupling of membrane proteins to the curvature of the ...

GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central physiological role in the regulation of cardiac function in both health and disease and thus represent one of ...

"G-protein-coupled receptors are ubiquitous in the function of cells in the body and help us to sense light, flavour and odour. They are also responsible for the human body's reactions to chemicals in ...

Thus, G-protein-coupled receptors can regulate NMDA receptor function indirectly through a PKC-dependent activation of the non-receptor tyrosine kinase (Src) signaling cascade.

Background—Desensitization of G protein–coupled receptors (GPCR) is emerging as an important feature of several cardiovascular diseases. G protein–coupled receptor kinase 2 (GRK2) plays a key role in ...

Everywhere you look, men are drinking matcha. How the green tea coffee alternative ended up at the center of a gendered debate.