 | Acta Crystallographica Section D Acta Crystallographica Section D BIOLOGICAL CRYSTALLOGRAPHY |
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![[Figure 1]](mn5020fig1mag.jpg)
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Figure 1
Ligand binding to MDM217–108 and MDM2_E69AK70A characterized by differential scanning fluorimetry (DSF) and fluorescence polarization anisotropy (FP). (a) Correlation of ΔTm for MDM217–108 and MDM2_E69AK70A. The ΔTm values for the two domains are the change in melting temperature that results from the addition of DMSO, p5315–29, Nutlin-3a, MI-63, compound 1 or compound 2 (see Supplementary Figs. S2 and S3 for the raw DSF data and for the structural formulae of the compounds used here, respectively, and Supplementary Table S1 for the derived Tm values). (b) Correlation of the Ki values of MDM217–108 and MDM2_E69AK70A, where the Ki values are the inhibition constants for interference with the binding of fluorescein-labelled p5315–29 to either MDM217–108 (x axis) or MDM2_E69AK70A (y axis) evaluated by fluorescence polarization anisotropy. Data are presented for the competitive ligands p5315–29, Nutlin-3a, MI-63, compound 1 and compound 2 (see Supplementary Figs. S4 and S3 for the raw FP data and the structural formulae of the compounds used here, respectively, and Supplementary Table S2 for the derived Ki values). (c, d) Raw FP data for the binding of fluorescein-labelled p5315–29 to either MDM217–108 (c) or MDM2_E69AK70A (d). |
![[Figure 1]](mn5020fig1.jpg)
| BIOLOGICAL CRYSTALLOGRAPHY |
ISSN: 1399-0047
