fig3

A dimethylbromobenzene-cysteine stapled peptide dual inhibitor of the p53-MDM2/MDMX interactions

Figure 3. The stapled peptides specifically targets intracellular complexes of p53/MDM2 and p53/MDMX. A: Schematic diagram for that stapled peptides can compete with p53 for MDM2 or MDMX binding; B and C: fluorescence polarization-based competitive binding assay of p53-MDM2/MDMX inhibitor (PMI) or stapled peptides to MDM2/p53 complex (B) and MDMX/p53 complex. For fluorescence polarization measurements at room temperature on a Tecan Infinite M2000 plate reader, FITC was covalently conjugated to the N-terminal of 15-29p53. Non-linear regression analyses were performed to give rise to IC50 values (mean ± SEM, n = 3); D: table for the results from B and C. Kd of PMI was cited from our previous reports, and Kd of SP1, SP2 and SP3 were calculated by the IC50 ratio between SPx to PMI

Hepatoma Research
ISSN 2454-2520 (Online) 2394-5079 (Print)

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