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. Author manuscript; available in PMC: 2022 Jul 5.
Published in final edited form as: Eur J Med Chem. 2021 Apr 4;219:113425. doi: 10.1016/j.ejmech.2021.113425

Figure 3.

Figure 3.

Mechanistic study of MDM2-p53 degradation induced by WB214. (A) MDM2 and p53 degradation induced by WB214 is dependent on CRBN and the proteasome. Cells were pre-treated with CRBN ligand lenalidomide (20 μM), proteasome inhibitor MG132 (5 μM), MDM2 inhibitor Ugi ligand 1 (10 μM) or WB138 (10 μM) for 1 h, followed by treatment with DMSO or WB214 for 6 h; (B) Evaluation of the binding affinity of compounds 1,11a and WB214 to MDM2 by a competitive fluorescent polarization (FP) assay; (C) Study of the ternary complex formation induced by WB156 and WB214 at 100 nM using proximity ligation assay (PLA); (D) Study of the ternary complex formation by time-resolved fluorescence energy transfer (TR-FRET).