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APR-246 overcomes resistance to cisplatin and doxorubicin in ovarian cancer cells

18 Jun 2015

Abstract excerpt

Two main causes of platinum resistance are mutation in the tumor suppressor gene TP53 and drug-induced increase in intracellular glutathione concentration. Mutations in TP53 occur in about 50% of human tumors. APR-246 (PRIMA-1(MET)) is the first clinical-stage compound that reactivates mutant p53 and induces apoptosis. APR-246 is a prodrug that is converted to the active compound methylene quinuclidinone (MQ), a...

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PMID: 26086967
DOI: 10.1038/cddis.2015.143

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APR-246 overcomes resistance to cisplatin and doxorubicin in ovarian cancer cellsPMID 26086967Read ↗

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APR-246 reactivates mutant p53 by targeting cysteines 124 and 277Semantic proximity Read ↗

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