Differential functional selectivity and downstream signaling bias of ghrelin receptor antagonists and inverse agonists

What is it about?

Here we identify previously unknown effects of known ligands on the signalling of the ghrelin receptor, a major receptor important in regulation of appetite and the body's metabolism. Considering the limited success in the clinical development of ghrelin receptor-targeted drugs so far, these findings provide a novel insight into the pharmacological characteristics of ligands binding to this receptor and their signalling bias. These findings have important implications in the design of novel, more selective drugs targeting this receptor with predictable functional outcome and selectivity for pre-clinical and clinical drug development in areas of obesity and anorexia.Together, these data add to the rich molecular pharmacology and complex biology of the ghrelin receptor.

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