Article
Small-Molecule Reactivation of Mutant p53 to Wild-Type-like p53 through the p53-Hsp40 Regulatory Axis.
Chemistry & biology - 17 Sept 2015
Hiraki Masatsugu, Hwang So-Young, Cao Shugeng, Ramadhar Timothy R, Byun Sanguine, Yoon Kyoung Wan, Lee Jung Hyun, Chu Kiki, Gurkar Aditi U, Kolev Vihren, Zhang Jianming, Namba Takushi, Murphy Maureen E, Newman David J, Mandinova Anna, Clardy Jon, Lee Sam W
Abstract excerpt
TP53 is the most frequently mutated gene in human cancer, and small-molecule reactivation of mutant p53 function represents an important anticancer strategy. A cell-based, high-throughput small-molecule screen identified chetomin (CTM) as a mutant p53 R175H reactivator. CTM enabled p53 to transactivate target genes, restored MDM2 negative regulation, and selectively inhibited the growth of cancer cells harboring...
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