Endocrine Abstracts

Motilin (M), erythromycin (EM) and ghrelin (G) are recognized as important regulators of gastrointestinal motor function in humans that are mediated by class I guanine nucleotide-binding protein (G protein)-coupled motilin receptor (MR) and growth hormone secretagogue receptor (GHSR). These receptors have also been demonstrated as clinically useful pharmacological targets. However, a molecular relationship between MR and GHSR activation has been unclear. We generated human MR ...

The motilin receptor (MLNR) belongs to a family of Class I G protein-coupled receptors, and is an important endogenous regulator of gastrointestinal motor function. Motilin and erythromycin (EM), two chemically distinct full agonists of the motilin receptor, bind to distinct regions of this receptor, while the action of these different chemical classes of agonists likely yields a common activation state of the cytosolic face of this receptor that is responsible for interaction...