Discovery of a potent and selective GPR120 agonist

B Shimpukade, BD Hudson, CK Hovgaard…

Index: Shimpukade, Bharat; Hudson, Brian D.; Hovgaard, Christine Kiel; Milligan, Graeme; Ulven, Trond Journal of Medicinal Chemistry, 2012 , vol. 55, # 9 p. 4511 - 4515

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Citation Number: 69

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 ...