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- W2079110726 abstract "The screening for treatment-induced enzyme activities offers the opportunity to discover important regulatory mechanisms and the identification of potential targets for anti-cancer therapies. A novel screening technique was applied to screen substrate peptide sequences for proteolytic activities up- or down-regulated by ionizing radiation in tumor cells. One specific substrate sequence was cleaved in control cell extracts but to a smaller extent in irradiated cell extracts and investigated in detail. Based on protease-class-specific inhibitory studies and cleavage site analysis a potent warhead-inhibitor was synthesized and used to identify the proteasome as the protease of interest. The investigated sequence shows high homology to a regulatory site of nucleoporin 50, an element of the nuclear pore complex, and site specific cleavage of nucleoporin 50 was determined in vitro suggesting a novel link between the ionizing radiation-regulated proteasome and nuclear protein shuttling." @default.
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- W2079110726 date "2010-01-01" @default.
- W2079110726 modified "2023-09-27" @default.
- W2079110726 title "Substrate screening identifies a novel target sequence for the proteasomal activity regulated by ionizing radiation" @default.
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- W2079110726 doi "https://doi.org/10.1002/pmic.200900162" @default.
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