Ghrelin and LEAP-2: Rivals in Energy Metabolism

Omar Al-Massadi, Timo Müller, Matthias Tschöp, Carlos Diéguez, Ruben Nogueiras

Research output: Contribution to journalReview articlepeer-review

45 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)685-694
Number of pages10
JournalTrends in Pharmacological Sciences
Volume39
Issue number8
DOIs
StatePublished - Aug 2018

Keywords

  • GH
  • GHSR1a
  • LEAP-2
  • food intake
  • ghrelin
  • metabolic syndrome

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