Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 7, Pages 345-349Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml100106c
Keywords
Diabetes; FFA1; FFAR1; GPR40; fatty acids; drug discovery
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Funding
- Danish Council for Independent Research/Technology and Production [09-070364]
- German Research Foundation (DFG) [UL140/7-1, GRK1302/1]
- Dr. Hilmer Foundation
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The free fatty acid 1 receptor (FFA1 or GPR40), which is highly expressed on pancreatic beta-cells and amplifies glucose-stimulated insulin secretion, has emerged as attractive target for the treatment of type 2 diabetes Several FFA1 agonists containing the para-substituted dihydrocinnamic acid moiety are known. We here present a structure-activity relationship study of this compound family suggesting that the central methyleneoxy linker is preferable for the smaller compounds whereas the central methyleneamine linker gives higher potency to the larger compounds. The study resulted in the discovery of the potent and selective full FFA1 agonist TUG-469 (29).
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