Article
The curcumin analog HO-3867 selectively kills cancer cells by converting mutant p53 protein to transcriptionally active wildtype p53.
The Journal of biological chemistry - 23 Mar 2018
Madan Esha, Parker Taylor M, Bauer Matthias R, Dhiman Alisha, Pelham Christopher J, Nagane Masaki, Kuppusamy M Lakshmi, Holmes Matti, Holmes Thomas R, Shaik Kranti, Shee Kevin, Kiparoidze Salome, Smith Sean D, Park Yu-Soon A, Gomm Jennifer J, Jones Louise J, Tomás Ana R, Cunha Ana C, Selvendiran Karuppaiyah, Hansen Laura A, Fersht Alan R, Hideg Kálmán, Gogna Rajan, Kuppusamy Periannan
Abstract excerpt
p53 is an important tumor-suppressor protein that is mutated in more than 50% of cancers. Strategies for restoring normal p53 function are complicated by the oncogenic properties of mutant p53 and have not met with clinical success. To counteract mutant p53 activity, a variety of drugs with the potential to reconvert mutant p53 to an active wildtype form have been developed. However, these drugs are associated...
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