Article
PRIMA-1 reactivates mutant p53 by covalent binding to the core domain.
Cancer cell - 5 May 2009
Lambert Jeremy M R, Gorzov Petr, Veprintsev Dimitry B, Söderqvist Maja, Segerbäck Dan, Bergman Jan, Fersht Alan R, Hainaut Pierre, Wiman Klas G, Bykov Vladimir J N
Abstract excerpt
Restoration of wild-type p53 expression triggers cell death and eliminates tumors in vivo. The identification of mutant p53-reactivating small molecules such as PRIMA-1 opens possibilities for the development of more efficient anticancer drugs. Although the biological effects of PRIMA-1 are well demonstrated, little is known about its molecular mechanism of action. We show here that PRIMA-1 is converted to...
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