Recent Advances in Development of GPR40 Modulators (FFA1/FFAR1): An Emerging Target for Type 2 Diabetes

Author(s): Nutan Sharma, Sunita Bhagat*, Tejpal Singh Chundawat.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 17 , Issue 11 , 2017

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Graphical Abstract:


Background: GPR40, an orphan G-protein coupled receptor that is activated by medium and long-chain fatty acids and is highly expressed in pancreatic islets, adipose depots and the gastrointestinal tract are involved in energy source recognition, absorption, storage and/or metabolism. Since its deorphanization in 2003, G-protein-coupled receptor GPR40 has emerged as a potential target for type II diabetes because it has been hypothesized to participate in the adverse effects of chronic fatty acid exposure on function of β-cell.

Results: This signifies that G-protein-coupled receptors have recently emerged as novel therapeutic targets in metabolic diseases, such as diabetes, obesity and the metabolic syndrome. Therefore it seems natural that GPR40 represents a potentially attractive target to best meet the need for novel treatments for Type II diabetes.

Conclusion: This review describes recent advances and novel drug discovery approaches in the antidiabetic area, focusing on GPR40 modulators which have been synthesized till date and their Structure-Activity Relationship (SAR).

Keywords: Agonists, antagonists, FFA1, FFAR1, GPR40, insulin, Type 2 diabetes.

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Article Details

Year: 2017
Page: [947 - 958]
Pages: 12
DOI: 10.2174/1389557517666170120152917
Price: $58

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