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. 2019 Jun 20;24(12):2292. doi: 10.3390/molecules24122292

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© 2019 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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MP-292 is a bona fide Mdm2 binder with on-target cellular activity. (A) MP-292 binds to recombinant Mdm2 in a host of biophysical assays, including competitive fluorescence polarization (left panel), isothermal titration calorimetry (middle panel), and surface plasmon resonance (right panel). (B) MP-292 shows cellular activity in a β-lactamase-based p53 reporter assay (left panel) but not in counterscreen assays, such as those probing for disruption in membrane integrity (lactate dehydrogenase release, middle panel), nor a β-lactamase based reporter-assay driven from a tetracycline-dependent promoter (p53 independent, right panel).