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Article

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

2 Apr 2013

Abstract excerpt

The p53 tumor suppressor is a potent transcription factor that plays a key role in the regulation of cellular responses to stress. It is controlled by its negative regulator MDM2, which binds directly to p53 and inhibits its transcriptional activity. MDM2 also targets p53 for degradation by the proteasome. Many tumors produce high levels of MDM2, thereby impairing p53 function. Restoration of p53 activity by...

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PMID: 24900694
DOI: 10.1021/ml4000657

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