Comparative subcellular distribution of the copper complexes of bleomycin-A2 and deglycobleomycin-A2.
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.
Kénani
A
A
Institute for Cancer Research, INSERM Unité 124, Lille, France.
Bailly
C
C
Houssin
R
R
Hénichart
J P
JP
D001761:Bleomycin / Q000737:chemistry / Q000493:pharmacokinetics* / Q000031:analogs & derivatives; D003300:Copper / Q000493:pharmacokinetics*; D006801:Humans; D007624:KB Cells; D013347:Subcellular Fractions / Q000378:metabolism*
D001761:Bleomycin; C033284:deglycobleomycin; D003300:Copper