GHS-1a Agonists That Effectively Stimulate Food Intake and Body Weight Gain

摘要

Ghrelin, a 28 amino acid octanoylated peptide, is an endogenous ligand for the growth hormone (GH) secretagogue (GHS-1a) receptor. In addition to its GH secretion effect, ghrelin enhances food intake and induces body weight gain. Due to its unique biological activities on appetite and positive energy balance, ghrelin is considered as a viable target for developing therapeutic agents for the treatment of cachexic and anorexic disorders. Previously, we reported the discovery of a novel pentapeptide that has higher GHS-la receptor binding affinity and longer plasma half-life than human ghrelin (h-ghrelin) [1]. Based on the discovery, recently we have synthesized new peptide agonists of the GHS-1 receptor.