Abstract
G-protein-coupled receptor 40 (GPR40), known as free fatty acid receptor 1, is mainly expressed in pancreatic β-cells and activated by medium- and long-chain fatty acids. Increasing evidence indicates that the activation of GPR40 in cells causes insulin secretion, and GPR40 has become an attractive therapeutic target for type 2 diabetes. Recently, certain novel GPR40 agonists have been identified that regulate glucose-stimulated insulin secretion, leading to the development of new drugs for the treatment of type 2 diabetes. In this review, we focus on progress in the physiological role of GPR40 and potential drugs targeting GPR40 over the past decade.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Animals
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Benzofurans / pharmacology
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Berberine / pharmacology
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Clinical Trials, Phase II as Topic
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Diabetes Mellitus, Type 2 / drug therapy
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Diabetes Mellitus, Type 2 / metabolism
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Fatty Acids, Nonesterified / physiology
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Humans
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Hypoglycemic Agents / pharmacology
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Insulin / metabolism*
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Insulin Secretion
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Ligands
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Molecular Targeted Therapy
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Receptors, G-Protein-Coupled / agonists
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Receptors, G-Protein-Coupled / physiology*
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Sulfones / pharmacology
Substances
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Benzofurans
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FFAR1 protein, human
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Fatty Acids, Nonesterified
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Hypoglycemic Agents
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Insulin
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Ligands
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Receptors, G-Protein-Coupled
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Sulfones
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TAK-875
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Berberine