Discovery of a potent and selective GPR120 agonist
Research output: Contribution to journal › Journal article › Research › peer-review
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Discovery of a potent and selective GPR120 agonist. / Shimpukade, Bharat; Hudson, Brian D; Hovgaard, Christine Kiel; Milligan, Graeme; Ulven, Trond.
In: Journal of Medicinal Chemistry, Vol. 55, No. 9, 2012, p. 4511-4515.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Discovery of a potent and selective GPR120 agonist
AU - Shimpukade, Bharat
AU - Hudson, Brian D
AU - Hovgaard, Christine Kiel
AU - Milligan, Graeme
AU - Ulven, Trond
PY - 2012
Y1 - 2012
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
VL - 55
SP - 4511
EP - 4515
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 9
ER -
ID: 189158956