Abstract
Cloning and characterization of the ghrelin receptor as a 7-transmembrane (7TM), G-protein-coupled receptor (GPCR) was first reported by Howard and his co-workers (1996). The ghrelin receptor was initially described as a growth hormone secretagogue receptor since (GHSR) this was the most well-established physiological function at that time. The natural endogenous agonist remained unknown until Kojima and his co-workers discovered (1999) the peptide hormone ghrelin. Afterward, the activity of ghrelin receptors was linked primarily with the regulation of appetite, adiposity, and energy expenditure as well as inducing of growth hormone secretion (Davenport et al. 2005; Kojima et al. 2001). Another important milestone in the pharmacological characterization of the ghrelin receptor was the discovery of its constitutive activity (Holst et al. 2003, 2004). This chapter will focus on the molecular basis of this phenomenon and its relevance in health and disease.
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