Document Detail

Is GPR119 agonism an appropriate treatment modality for the safe amelioration of metabolic diseases?
MedLine Citation:
PMID:  23442069     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: GPR119 is a recently deorphanised G-protein coupled receptor which has been suggested to be important in mediating systemic metabolic homeostasis. Research to date has primarily focused on the ability of GPR119 to promote euglycaemia and thus as a therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Indeed, previous studies have shown that GPR119 promotes glucose-stimulated insulin secretion, pancreatic β-cell function and glucagon-like peptide-1 release, all of which provide valid mechanisms through which GPR119 may improve systemic glucose homeostasis.
AREAS COVERED: In the current review, the authors provide a brief overview of the known functions of GPR119 and then discuss the novel potential for GPR119 to regulate metabolic function in skeletal and cardiac muscle and how this may translate to improvements or impairments in systemic health.
EXPERT OPINION: GPR119 is largely purported as being anti-diabetic and has been rapidly progressed to clinical trials, mainly as anti-diabetic agents. However, emerging data suggest that this class of agonists may have a detrimental effect at the level of the muscle. This may potentiate the development and progression of metabolic diseases such as T2DM. Therefore, further research is required before GPR119 receptor agonists can be prescribed with confidence as an anti-diabetic agent.
Lauren M Cornall; Michael L Mathai; Deanne H Hryciw; Andrew J McAinch
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Review     Date:  2013-02-27
Journal Detail:
Title:  Expert opinion on investigational drugs     Volume:  22     ISSN:  1744-7658     ISO Abbreviation:  Expert Opin Investig Drugs     Publication Date:  2013 Apr 
Date Detail:
Created Date:  2013-03-14     Completed Date:  2013-08-26     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9434197     Medline TA:  Expert Opin Investig Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  487-98     Citation Subset:  IM    
Victoria University, College of Health and Biomedicine, Biomedical and Lifestyle Diseases Unit, Melbourne, Australia.
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MeSH Terms
Metabolic Diseases / drug therapy,  metabolism*
Muscle, Skeletal / metabolism
Myocardium / metabolism
Receptors, G-Protein-Coupled / agonists,  metabolism*
Reg. No./Substance:
0/Gpr119 protein, mouse; 0/Receptors, G-Protein-Coupled

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