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. Author manuscript; available in PMC: 2021 Dec 24.
Published in final edited form as: J Med Chem. 2020 Dec 16;63(24):16012–16027. doi: 10.1021/acs.jmedchem.0c01874

Figure 5.

Figure 5.

Effects of truncated 1′-homologated adenosine derivatives on PPARδ coregulation. (A) TR-FRET-based PPARδ corepression assay was performed using fluorescein-SMRT corepressor peptide. A PPARδ agonist 27 and a PPARδ antagonist 28 were used as positive or negative controls. The degree of the recruiting corepressor to PPARγ-LBD was normalized to % corepression. (B) TR-FRET-based PPARδ coactivation assay was performed using coactivator C33. (C) Concentration-dependent effects of 4d and 4p on the PPARδ corepression were investigated. (D) Pearson’s correlation coefficient (R2) between the PPARδ corepression activity and the level of relative adiponectin secretion-promoting activity was calculated using the Pearson correlation analysis. (E) Effects of PPARδ agonist 27 (1 μM) on PPARδ antagonism of 4d (10 μM) and 28 (1 μM). Results are the mean ± SD of three measurements (n = 3); (*) p ≤ 0.05 and (**) p ≤ 0.01.