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

Cell Death Dis. 2015; 
MohellN,AlfredssonJ,FranssonÅ,UustaluM,ByströmS,GullboJ,HallbergA,BykovV J N,BjörklundU,Wima
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Biochemicals Human cancer tissue samples were obtained from Capital Biosciences (Rockville, MD, USA) and Genscript (Piscataway, NJ, USA). Get A Quote

摘要

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 Michael acceptor that binds to cysteine residues in mutant p53 and restores its wild-type conformation. Here, we show that MQ also binds to cysteine in glutathione, thus decreasing intracellular free glutathione concentration. We also show that treatment with APR-246 completely restores the cispla... More

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