Article Figures & Data
Figures
- Fig. 1.
SPR analysis of atorvastatin, rosuvastatin, and CITCO binding to hCAR/hRXRα-LBD heterodimer. Different concentrations (1.56, 3.125, 12.5, 25, and 50 µM for CITCO and 6, 12.5, 25, 50, 75, 100, and 150 µM for atorvastatin and rosuvastatin) of analytes were tested for the binding (left panels). The binding curves (right panels) were generated by fitting the steady-state response levels at the end of the association phase versus the concentration of the injected analyte. The KD values were obtained by fitting the data to the steady-state affinity model. For each analyte six or seven independent titration experiments were performed.
Tables
- TABLE 1
KD values and theoretical and measured maximal responses of atorvastatin, rosuvastatin, and CITCO binding to hCAR/hRXRα-LBD heterodimer as measured by surface plasmon resonance and by scores of ligand-based (CAR pharmacophore) and structure-based (CAR score docking) in silico calculations
Compound KD (µM) CAR Maximal Response Score Docking Pharmacophore Theoretical Measured Atorvastatin 0.225 ± 0.06 73.18 2.07 84 251 Rosuvastatin 0.144 ± 0.03 67.09 — 70 86 CITCO 0.045 ± 0.04 63.02 — 30 74
Data Supplement
- Supplemental Data -
Supplemental methods, 3 figures, 1 table.
- Supplemental Data -
In this issue
Statins Are Ligands of Human CAR/RXRα Complex
