A thiol‐bound drug reservoir enhances APR‐246‐induced mutant p53 tumor cell death

A thiol‐bound drug reservoir enhances APR‐246‐induced mutant p53 tumor cell death

Abstract 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 cl...

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Bibliographic Details
Main Authors: Sophia Ceder, Sofi E Eriksson, Emarndeena H Cheteh, Swati Dawar, Mariana Corrales Benitez, Vladimir J N Bykov, Kenji M Fujihara, Mélodie Grandin, Xiaodun Li, Susanne Ramm, Corina Behrenbruch, Kaylene J Simpson, Frédéric Hollande, Lars Abrahmsen, Nicholas J Clemons, Klas G Wiman
Format: Article
Language:English
Published: Springer Nature 2020-12-01
Series:EMBO Molecular Medicine
Subjects:
APR‐246
Eprenetapopt
glutathione
MRP1
p53
Online Access:https://doi.org/10.15252/emmm.201910852
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