Rescue of the apoptotic-inducing function of mutant p53 by small molecule RITA
作者： Carolyn Y. Zhao , Vera Grinkevich , Fedor Nikulenkov , Wenjie Bao , Galina Selivanova
DOI: 10.4161/CC.9.9.11545
关键词:
摘要: Expression of mutant p53 correlates with poor prognosis in many tumors, therefore strategies aimed at reactivation are likely to provide important benefits for treatment tumors that resistant chemotherapy and radiotherapy. We have previously identified characterized a small molecule RITA which binds induces conformational change prevents the binding several inhibitors, including its own destructor MDM2. In this way, rescues tumor suppression function wild type p53. Here, we demonstrate suppressed growth induced apoptosis human cell lines diverse origin carrying proteins. restored transcriptional transactivation transrepression hot spot mutants. The ability rescue activity different mutants suggests generic mechanism action. Thus, is promising lead development anti-cancer drugs reactivate suppressor cancer cells irrespective whether they express or
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