期刊
TRENDS IN PHARMACOLOGICAL SCIENCES
卷 39, 期 8, 页码 685-694出版社
ELSEVIER SCIENCE LONDON
DOI: 10.1016/j.tips.2018.06.004
关键词
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资金
- Ministerio de Economia y Competitividad [BFU2017-55871-P, BFU2015-70664R]
- Xunta de Galicia [2015-CP080, 2016-PG057]
- Centro de Investigacion Biomedica en Red (CIBER) de Fisiopatologia de la Obesidad y Nutricion (CIBERobn)
- European Community [ERC-2011-StG-OBESITY53-281408]
- FEDER funds
- ISCIII/SERGAS [CD14/00091]
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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