Discovery of a potent and selective GPR120 agonist

Bharat Shimpukade; Brian D Hudson; Christine Kiel Hovgaard; Graeme Milligan; Trond Ulven

doi:10.1021/jm300215x

Discovery of a potent and selective GPR120 agonist

Bharat Shimpukade, Brian D Hudson, Christine Kiel Hovgaard, Graeme Milligan, Trond Ulven

112 Citations (Scopus)

Abstract

GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.

Original language	English
Journal	Journal of Medicinal Chemistry
Volume	55
Issue number	9
Pages (from-to)	4511-4515
Number of pages	5
ISSN	0022-2623
DOIs	https://doi.org/10.1021/jm300215x
Publication status	Published - 10 May 2012

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10.1021/jm300215x

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abstract = "GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.",

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AU - Shimpukade, Bharat

AU - Hudson, Brian D

AU - Hovgaard, Christine Kiel

AU - Milligan, Graeme

AU - Ulven, Trond

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Y1 - 2012/5/10

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AB - GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.

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DO - 10.1021/jm300215x

M3 - Journal article

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Discovery of a potent and selective GPR120 agonist

Abstract

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