Source:http://linkedlifedata.com/resource/pubmed/id/19562648
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2009-6-29
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pubmed:abstractText |
Type 2 diabetes (T2D) and associated obesity have reached epidemic proportions, and there is an increasing need for orally effective agents that regulate glucose homeostasis with a concurrent reduction in body weight. GPR119, a class-A (rhodopsin-like) G protein-coupled receptor, expressed primarily in the human pancreas and gastrointestinal tract, has attracted considerable interest as a T2D drug target in the last three to five years. The activation of GPR119 increases the intracellular accumulation of cAMP, leading to enhanced glucose-dependent insulin secretion and increased levels of the incretin hormones GLP-1 (glucagon-like peptide 1) and GIP (glucose-dependent insulinotropic peptide). In rodent models, orally available GPR119-specific agonists have been shown to attenuate blood glucose levels with a simultaneous body weight loss. This review summarizes the research leading to the identification of GPR119 as a potential drug target for T2D and related metabolic disorders. In addition, an overview of the recent progress made in the discovery of orally active GPR119 agonists is provided.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/GPR119 protein, human,
http://linkedlifedata.com/resource/pubmed/chemical/Hypoglycemic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, G-Protein-Coupled,
http://linkedlifedata.com/resource/pubmed/chemical/Small Molecule Libraries
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pubmed:status |
MEDLINE
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pubmed:month |
Jul
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pubmed:issn |
2040-3437
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
519-32
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pubmed:meshHeading |
pubmed-meshheading:19562648-Animals,
pubmed-meshheading:19562648-Clinical Trials as Topic,
pubmed-meshheading:19562648-Cyclic AMP,
pubmed-meshheading:19562648-Diabetes Mellitus, Type 2,
pubmed-meshheading:19562648-Drug Design,
pubmed-meshheading:19562648-Humans,
pubmed-meshheading:19562648-Hypoglycemic Agents,
pubmed-meshheading:19562648-Metabolic Diseases,
pubmed-meshheading:19562648-Molecular Structure,
pubmed-meshheading:19562648-Receptors, G-Protein-Coupled,
pubmed-meshheading:19562648-Small Molecule Libraries
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pubmed:year |
2009
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pubmed:articleTitle |
GPR119 agonists: a promising new approach for the treatment of type 2 diabetes and related metabolic disorders.
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pubmed:affiliation |
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. unmesh.shah@spcorp.com
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pubmed:publicationType |
Journal Article,
Review
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