Article
Synthetic metallochaperone ZMC1 rescues mutant p53 conformation by transporting zinc into cells as an ionophore.
Molecular pharmacology - 1 May 2015
Blanden Adam R, Yu Xin, Wolfe Aaron J, Gilleran John A, Augeri David J, O'Dell Ryan S, Olson Eric C, Kimball S David, Emge Thomas J, Movileanu Liviu, Carpizo Darren R, Loh Stewart N
Abstract excerpt
p53 is a Zn(2+)-dependent tumor suppressor inactivated in >50% of human cancers. The most common mutation, R175H, inactivates p53 by reducing its affinity for the essential zinc ion, leaving the mutant protein unable to bind the metal in the low [Zn(2+)]free environment of the cell. The exploratory cancer drug zinc metallochaperone-1 (ZMC1) was previously demonstrated to reactivate this and other Zn(2+)-binding...
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