Pharmacological Modulation of Ghrelin to Induce Weight Loss: Successes and Challenges

Overview

Journal Curr Diab Rep

Publisher Current Science

Specialty Endocrinology

Date 2019 Sep 12

PMID 31506846

Citations 17

Authors

Martha A Schalla

Andreas Stengel

Affiliations

Soon will be listed here.

Abstract

Purpose Of Review: Obesity is affecting over 600 million adults worldwide and has numerous negative effects on health. Since ghrelin positively regulates food intake and body weight, targeting its signaling to induce weight loss under conditions of obesity seems promising. Thus, the present work reviews and discusses different possibilities to alter ghrelin signaling.

Recent Findings: Ghrelin signaling can be altered by RNA Spiegelmers, GHSR/Fc, ghrelin-O-acyltransferase inhibitors as well as antagonists, and inverse agonists of the ghrelin receptor. PF-05190457 is the first inverse agonist of the ghrelin receptor tested in humans shown to inhibit growth hormone secretion, gastric emptying, and reduce postprandial glucose levels. Effects on body weight were not examined. Although various highly promising agents targeting ghrelin signaling exist, so far, they were mostly only tested in vitro or in animal models. Further research in humans is thus needed to further assess the effects of ghrelin antagonism on body weight especially under conditions of obesity.

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