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Abstract
Background: Ghrelin is a stomach-derived octanoylated hormone that has been implicated in body weight regulation and glucose homeostasis. It mediates its pharmacological activities primarily through the ghrelin receptor (GhR). The discovery of small molecule GhR antagonists and other biological agents that can modulate ghrelin activity has attracted considerable interest over the past few years. Objectives: This review summarizes the role of ghrelin and its receptor in regulating body weight and glucose homeostasis and describes ghrelin system modulators that have appeared in the patent literature from 2002 to 2008. Results/conclusions: A variety of different agents that alter ghrelin activity have been disclosed, including peptidyl and non-peptidyl receptor antagonists as well as biological agents such as monoclonal antibodies, catalytic activating antibodies, vaccines and Spiegelmers. Many of these agents have been shown to decrease food intake and reduce body weight, although the effect of these modulators on glucose homeostasis has yet to be examined.