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Ghrelin and LEAP-2: Rivals in energy metabolism.
Trends Pharmacol. Sci. 39, 685-694 (2018)
Liver-expressed antimicrobial peptide 2 (LEAP-2), the endogenous noncompetitive allosteric antagonist of the growth hormone secretagogue receptor 1a (GHSR1a), was recently identified as a key endocrine factor regulating systemic energy metabolism. This antagonist impairs the ability of ghrelin to activate GHSR1a and diminishes ghrelin-induced Ca2+ release in vitro. The physiological relevance of the molecular LEAP-2-GHSR1a interaction was subsequently demonstrated in vivo. LEAP-2 is therefore a promising therapeutic target in the treatment of obesity and other metabolic diseases. Here, we discuss not only the current understanding of LEAP-2 in metabolic regulation, but also the potential of this peptide in the treatment of obesity and other diseases that involve dysregulation of the ghrelin system.
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Publication type Article: Journal article
Document type Review
Keywords Gh ; Ghsr1a ; Leap-2 ; Food Intake ; Ghrelin ; Metabolic Syndrome; Des-acyl Ghrelin; Hormone Secretagogue Receptor; Healthy Older-adults; Diet-induced Obesity; Growth-hormone; Food-intake; Double-blind; Weight-loss; Glucose-metabolism; Gastric Bypass
Institute(s) Institute of Diabetes and Obesity (IDO)