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Review
. 2013 Dec;70(24):4759-70.
doi: 10.1007/s00018-013-1419-9. Epub 2013 Jul 14.

The therapeutic potential of GPR43: a novel role in modulating metabolic health

Lauren M Cornall  1 , Michael L Mathai, Deanne H Hryciw, Andrew J McAinch
Affiliations
Review

The therapeutic potential of GPR43: a novel role in modulating metabolic health

Lauren M Cornall et al. Cell Mol Life Sci. 2013 Dec.

Abstract

GPR43 is a receptor for short-chain fatty acids. Preliminary data suggest a putative role for GPR43 in regulating systemic health via processes including inflammation, carcinogenesis, gastrointestinal function, and adipogenesis. GPR43 is involved in secretion of gastrointestinal peptides, which regulate appetite and gastrointestinal motility. This suggests GPR43 may have a role in weight control. Moreover, GPR43 regulates plasma lipid profile and inflammatory processes, which further indicates that GPR43 could have the ability to modulate the etiology and pathogenesis of metabolic diseases such as obesity, type 2 diabetes mellitus, and cardiovascular disease. This review summarizes the current evidence regarding the ability of GPR43 to mediate both systemic and tissue specific functions and how GPR43 may be modulated in the treatment of metabolic disease.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Fig. 1
Fig. 1
Proposed interplay of GPR43-mediated effects on metabolic homeostasis. Proposed pathways that represent the complexity with which GPR43 has the ability to regulate both tissue-specific and systemic metabolic function. These roles indicate GPR43 as a drug target for the treatment of metabolic diseases such as obesity, type 2 diabetes mellitus, and cardiovascular disease. Solid lines represent a direct effect of GPR43; Broken lines represent an indirect or secondary effect of GPR43 activation on metabolic function. The sum of these direct and indirect mechanisms provides multiple points of cross-talk between the distinct effects, suggesting that by targeting one aspect of GPR43 functionality it is likely to modulate other related pathways. 5-HT 5-hydroxytryptamine, Ad adiponectin, GLP-1 glucagon-like peptide 1, Lep leptin, MAPK mitogen activated protein kinase, PYY peptide YY
See this image and copyright information in PMC

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