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 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	Journal of Medicinal Chemistry
Vol/bind	55
Udgave nummer	9
Sider (fra-til)	4511-4515
Antal sider	5
ISSN	0022-2623
DOI	https://doi.org/10.1021/jm300215x
Status	Udgivet - 10 maj 2012

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10.1021/jm300215x

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AU - Shimpukade, Bharat

AU - Hudson, Brian D

AU - Hovgaard, Christine Kiel

AU - Milligan, Graeme

AU - Ulven, Trond

PY - 2012/5/10

Y1 - 2012/5/10

N2 - 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.

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.

U2 - 10.1021/jm300215x

DO - 10.1021/jm300215x

M3 - Journal article

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VL - 55

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JF - Journal of Medicinal Chemistry

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Discovery of a potent and selective GPR120 agonist

Abstract

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