Small molecule inhibitors of Mdm2 E3 ubiquitin ligase activity
Dickens, Michael (2011) Small molecule inhibitors of Mdm2 E3 ubiquitin ligase activity. PhD thesis, University of Nottingham.
Half of cancers retain wild type p53 but have alterations in the pathways involved in p53 regulation. Murine double minute 2 (Mdm2) regulates p53 by acting as an E3 ubiquitin ligase, which tags p53 for degradation through the proteasome. A small molecule inhibitor, a 5-deazaflavin analogue, has previously been identified by high throughput screening to inhibit Mdm2 E3 ubiquitin ligase activity, thereby reactivating apoptotic function of p53 selectively in cancer cells.
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