Abstract
Appetite regulation is highly complex and involves a large number of orexigenic and anorexigenic peptide hormones. These are small, processed, secreted peptides derived from larger prepropeptide precursors. These peptides are important targets for the development of therapeutics for obesity, a global health epidemic. As a case study, we consider the ghrelin axis. The ghrelin axis is likely to be a particularly useful drug target, as it also plays a role in energy homeostasis, adipogenesis, insulin regulation and reward associated with food intake. Ghrelin is the only known circulating gut orexigenic peptide hormone. As it appears to play a role in diet-induced obesity, blocking the action of ghrelin is likely to be effective for treating and preventing obesity. The ghrelin peptide has been targeted using a number of approaches, with ghrelin mirror-image oligonucleotides (Spiegelmers) and immunotherapy showing some promise. The ghrelin receptor, the growth hormone secretagogue receptor, may also provide a useful target and a number of antagonists and inverse agonists have been developed. A particularly promising new target is the enzyme which octanoylates ghrelin, ghrelin O-acyltransferase (GOAT), and drugs that inhibit GOAT are likely to circumvent pharmacological issues associated with approaches that directly target ghrelin or its receptor.
Keywords: Appetite, peptide hormone, ghrelin, GHSR, GOAT, epidemic, oligonucleotides, immunotherapy, Spiegelmers, cryptide
Current Pharmaceutical Design
Title: Ghrelin and the Brain-gut Axis as a Pharmacological Target for Appetite Control
Volume: 18 Issue: 6
Author(s): Inge Seim, Magdy El-Salhy, Trygve Hausken, Doris Gundersen and Lisa Chopin
Affiliation:
Keywords: Appetite, peptide hormone, ghrelin, GHSR, GOAT, epidemic, oligonucleotides, immunotherapy, Spiegelmers, cryptide
Abstract: Appetite regulation is highly complex and involves a large number of orexigenic and anorexigenic peptide hormones. These are small, processed, secreted peptides derived from larger prepropeptide precursors. These peptides are important targets for the development of therapeutics for obesity, a global health epidemic. As a case study, we consider the ghrelin axis. The ghrelin axis is likely to be a particularly useful drug target, as it also plays a role in energy homeostasis, adipogenesis, insulin regulation and reward associated with food intake. Ghrelin is the only known circulating gut orexigenic peptide hormone. As it appears to play a role in diet-induced obesity, blocking the action of ghrelin is likely to be effective for treating and preventing obesity. The ghrelin peptide has been targeted using a number of approaches, with ghrelin mirror-image oligonucleotides (Spiegelmers) and immunotherapy showing some promise. The ghrelin receptor, the growth hormone secretagogue receptor, may also provide a useful target and a number of antagonists and inverse agonists have been developed. A particularly promising new target is the enzyme which octanoylates ghrelin, ghrelin O-acyltransferase (GOAT), and drugs that inhibit GOAT are likely to circumvent pharmacological issues associated with approaches that directly target ghrelin or its receptor.
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Cite this article as:
Seim Inge, El-Salhy Magdy, Hausken Trygve, Gundersen Doris and Chopin Lisa, Ghrelin and the Brain-gut Axis as a Pharmacological Target for Appetite Control, Current Pharmaceutical Design 2012; 18 (6) . https://dx.doi.org/10.2174/138161212799277806
DOI https://dx.doi.org/10.2174/138161212799277806 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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