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We have compared the cellular uptake and subcellular localization of 14C-labeled bleomycin-A2 (BLM) and deglycobleomycin-A2 in living KB3 cells. Both drugs exhibit poor internalization into cells but reveal significantly different intracellular distribution, with low and high accumulation into the cell nuclei for BLM and deglyco-BLM, respectively. The results indicate that the carbohydrate chain does not constitute a limiting factor for BLM permeation and is directly implicated in the intracellular distribution of the drug into cells.
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