Small-molecule inhibitors of the p53-HDM2 interaction for the treatment of cancer

Abstract excerpt

BACKGROUND: The hdm2 oncogene product, HDM2 (also known as MDM2), is an ubiquitin protein ligase that suppresses the transcriptional activity of the tumor suppressor p53 and promotes its degradation. Approximately 50% of all human tumors harbor mutations or deletions in the TP53 gene. In the remaining half of all human cancers that express the wild-type protein, aberrations of p53 regulators such as HDM2 account...

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