Article
A thiol-bound drug reservoir enhances APR-246-induced mutant p53 tumor cell death.
EMBO molecular medicine - 5 Feb 2021
Ceder Sophia, Eriksson Sofi E, Cheteh Emarndeena H, Dawar Swati, Corrales Benitez Mariana, Bykov Vladimir J N, Fujihara Kenji M, Grandin Mélodie, Li Xiaodun, Ramm Susanne, Behrenbruch Corina, Simpson Kaylene J, Hollande Frédéric, Abrahmsen Lars, Clemons Nicholas J, Wiman Klas G
Abstract excerpt
The tumor suppressor gene TP53 is the most frequently mutated gene in cancer. The compound APR-246 (PRIMA-1Met/Eprenetapopt) is converted to methylene quinuclidinone (MQ) that targets mutant p53 protein and perturbs cellular antioxidant balance. APR-246 is currently tested in a phase III clinical trial in myelodysplastic syndrome (MDS). By in vitro, ex vivo, and in vivo models, we show that combined treatment...
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