Figure 8 | Scientific Reports

Figure 8

From: Selective targeting of nuclear receptor FXR by avermectin analogues with therapeutic effects on nonalcoholic fatty liver disease

Figure 8

Functional correlation of the avermectins/FXR interactions.

(a–d) Molecular determinants of the interaction between FXR with avermectins. Overlays of avermectin (green) and GW4064 (salmon red) in the FXR structure (grey). The selected residues important for ligand interaction are shown in stick representation with wild-type and mutant depicted in white and blue, respectively. The hydrogen bonds are shown with arrows. The potential hydrophobic interactions, if the corresponding mutations are made as indicated in (e), are shown in dashed lines. (e) Differential effects of mutations of key FXR residues on its transcriptional activity in response to 1 μM avermectin analogues in reporter assays. Values are the means ± SEM of three independent experiments.

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