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. 2017 Oct 23;7:13741. doi: 10.1038/s41598-017-14096-3

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© The Author(s) 2017

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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Species selectivity of FFA2 antagonists for human versus mouse ortholog is determined by the identity of residue 65 in FFA2. Receptors of interest were expressed in-frame with eYFP in Flp-In TREx 293 cells. (a) The ability of varying concentrations of C3 () and compound 1 (●) to promote production of inositol monophosphates was assessed. (b) The capacity of varying concentrations of either GLPG0974 (●) or CATPB () to inhibit inositol monophosphate production induced by EC₈₀ concentrations of C3 at either hFFA2 (●) or mFFA2 (○) was assessed. (c) Chemical structures of GLPG0974 and CATPB are shown. (d) Docking of GLPG0974 (di) and CATPB (dii) into a homology model of hFFA2 with focus on the potential interaction of each ligand with Lys⁶⁵ (residue 2.60). The insert highlights overlapping poses of GLPG0974 (cyan) and CATPB (green) within the binding pocket despite their structural differences (e). The ability of varying concentrations of C3 () and compound 1 (●) to promote generation of inositol monophosphates in Flp-In TREx 293 cells induced to express Lys⁶⁵Arg (●), Lys⁶⁵Ala (■), and Lys⁶⁵Glu (▲) hFFA2 is illustrated. (f,g) The ability of GLPG0974 (f) or CATPB (g) to inhibit inositol monophosphate production induced by EC₈₀ concentrations of compound 1 at wild type and each of Lys⁶⁵Arg (○), Lys⁶⁵Ala (□), and Lys⁶⁵Glu (△) hFFA2 is shown. (h) The ability of GLPG0974 (●) or CATPB () to inhibit inositol monophosphate production induced by C3 at wild type (dotted line) and Arg⁶⁵Lys (●) mFFA2 is illustrated.

Inline graphic — Species selectivity of FFA2 antagonists for human versus mouse ortholog is determined by the identity of residue 65 in FFA2. Receptors of interest were expressed in-frame with eYFP in Flp-In TREx 293 cells. (a) The ability of varying concentrations of C3 () and compound 1 (●) to promote production of inositol monophosphates was assessed. (b) The capacity of varying concentrations of either GLPG0974 (●) or CATPB () to inhibit inositol monophosphate production induced by EC₈₀ concentrations of C3 at either hFFA2 (●) or mFFA2 (○) was assessed. (c) Chemical structures of GLPG0974 and CATPB are shown. (d) Docking of GLPG0974 (di) and CATPB (dii) into a homology model of hFFA2 with focus on the potential interaction of each ligand with Lys⁶⁵ (residue 2.60). The insert highlights overlapping poses of GLPG0974 (cyan) and CATPB (green) within the binding pocket despite their structural differences (e). The ability of varying concentrations of C3 () and compound 1 (●) to promote generation of inositol monophosphates in Flp-In TREx 293 cells induced to express Lys⁶⁵Arg (●), Lys⁶⁵Ala (■), and Lys⁶⁵Glu (▲) hFFA2 is illustrated. (f,g) The ability of GLPG0974 (f) or CATPB (g) to inhibit inositol monophosphate production induced by EC₈₀ concentrations of compound 1 at wild type and each of Lys⁶⁵Arg (○), Lys⁶⁵Ala (□), and Lys⁶⁵Glu (△) hFFA2 is shown. (h) The ability of GLPG0974 (●) or CATPB () to inhibit inositol monophosphate production induced by C3 at wild type (dotted line) and Arg⁶⁵Lys (●) mFFA2 is illustrated.