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Chemical Inhibition Of Caax Protease Activity Disrupts Yeast Ras Localization, Surya P. Mandahar, Emily R. Hildebrandt, William H. Jacobsen, George M. Santangelo, Walter K. Schmidt
Chemical Inhibition Of Caax Protease Activity Disrupts Yeast Ras Localization, Surya P. Mandahar, Emily R. Hildebrandt, William H. Jacobsen, George M. Santangelo, Walter K. Schmidt
Faculty Publications
Proteins possessing a C-terminal CaaX motif, such as the Ras GTPases, undergo extensive post-translational modification that includes attachment of an isoprenoid lipid, proteolytic processing and carboxylmethylation. Inhibition of the enzymes involved in these processes is considered a cancer-therapeutic strategy. We previously identified nine in vitro inhibitors of the yeast CaaX protease Rce1p in a chemical library screen (Manandhar et al., 2007). Here, we demonstrate that these agents disrupt the normal plasma membrane distribution of yeast GFP-Ras reporters in a manner that pharmacologically phenocopies effects observed upon genetic loss of CaaX protease function. Consistent with Rce1p being the in vivo target …