Ghrelin, a gastrointestinal hormone, functions as an endogenous ligand for the growth hormone secretagogue receptor (GHS-R). It comprises 28 amino acids, of which the Ser-3 residue is post-translationally modified by the addition of octanoyl acid. Ghrelin stimulates feeding and the secretion of growth hormone; it is also thought to function in energy conservation. Here, we provide an overview of the discovery of ghrelin, its pathophysiological significance, and the mechanism of ghrelin-induced feeding. (C) 2012 Asian Oceanian Association for the Study of Obesity. Published by Elsevier Ltd. All rights reserved.