Ontology highlight
ABSTRACT:
SUBMITTER: Hiraki M
PROVIDER: S-EPMC4670040 | biostudies-literature | 2015 Sep
REPOSITORIES: biostudies-literature
Chemistry & biology 20150827 9
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 mutant p53 R175H in vitro and in vivo. We found that CTM binds to Hsp40 and increase ...[more]