Cross-Species Differential Plasma Protein Binding of MBX-102/JNJ39659100: A Novel PPAR- Agonist
Figure 6
Displacement of NCOR corepressor peptide from PPAR-γ ligand-binding domain by MBX-102 acid
in the presence of human serum compared to mouse and rat serum. MBX-102
acid induced displacement of NCOR corepressor peptide from human PPAR-γ ligand-binding domain in the presence
of 40% (v/v) human (H), mouse (M), or rat (R) serum. Normalized FRET assay data
are expressed as the percentage of maximum signal (“percentage of maximal signal,” as described
in Figure 2(a)).
The dose-response curves shown are from a representative experiment. Values are
IC50 (M) determined from 3 experiments and shown as the mean ± SD.
FC is the IC50 fold change of mouse or rat compared to human (*** = by ANOVA with
Tukey post hoc test).
