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• W2809969055 abstract "The free fatty acid receptor 1 (FFA1) enhances the glucose-stimulated insulin secretion without the risk of hypoglycemia. However, most of FFA1 agonists have a common biphenyl moiety, leading to a relative deprivation in structure types. Herein, we describe the exploration of non-biphenyl scaffold based on the co-crystal structure of FFA1 to increase additional interactions with the lateral residues, which led to the identification of lead compounds 3 and 9. In induced-fit docking study, compound 3 forms an edge-on interaction with Trp150 by slightly rotating the indole ring of Trp150, and compound 9 has additional hydrogen bond and δ-π interactions with Leu135, which demonstrated the feasibility of our design strategy. Moreover, lead compounds 3 and 9 revealed improved polar surface area compared to GW9508, and have considerable hypoglycemic effects in mice. This structure-based study might inspire us to design more promising FFA1 agonists by increasing additional interactions with the residues outside of binding pocket." @default.
• W2809969055 created "2018-07-10" @default.
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• W2809969055 date "2018-10-01" @default.
• W2809969055 modified "2023-10-17" @default.
• W2809969055 title "Structure-based design of free fatty acid receptor 1 agonists bearing non-biphenyl scaffold" @default.
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• W2809969055 doi "https://doi.org/10.1016/j.bioorg.2018.06.039" @default.
• W2809969055 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29980115" @default.
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