Ghrelin and ghrelin receptor inhibitors: agents in the treatment of obesity

Background: Current medical treatment of obesity is highly ineffective. Soon after its discovery as the endogenous ligand for the growth hormone secretagogue-receptor (GHS-R), ghrelin was shown to stimulate food intake (including in humans) and promote body weight gain and adipogenesis. Objectives: This review discusses the role of the ghrelin/GHS-R pathway in energy homeostasis regulation and its role as a novel molecular target for the treatment of obesity. Methods: Medline was searched for relevant articles published in English. Results/conclusion: A large series of animal studies shows that inhibition of the ghrelin/GHS-R pathway reduces food intake, body weight and adiposity, through reduction of appetite and augmentation of energy expenditure and fat catabolism. This suggests that inhibition of this novel pathway may be used to treat/prevent obesity and its complications.