Article
APR-246 potently inhibits tumour growth and overcomes chemoresistance in preclinical models of oesophageal adenocarcinoma.
Gut - 1 Oct 2015
Liu David S H, Read Matthew, Cullinane Carleen, Azar Walid J, Fennell Christina M, Montgomery Karen G, Haupt Sue, Haupt Ygal, Wiman Klas G, Duong Cuong P, Clemons Nicholas J, Phillips Wayne A
Abstract excerpt
OBJECTIVES: p53 is a critical tumour suppressor and is mutated in 70% of oesophageal adenocarcinomas (OACs), resulting in chemoresistance and poor survival. APR-246 is a first-in-class reactivator of mutant p53 and is currently in clinical trials. In this study, we characterised the activity of APR-246 and its effect on p53 signalling in a large panel of cell line xenograft (CLX) and patient-derived xenograft...
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