Abstract
Substrates containing doxorubicin (DOX), paclitaxel (taxol), and mitomycin C (MMC) attached to the cathepsin B-sensitive dipeptide Phe-Lys via a self-immolative spacer were prepared as model compounds for internalizing anticancer immunoconjugates. Cathepsin B-mediated release rates of free drug, rat liver lysosomal susceptibility and human plasma stability were measured for each.
MeSH terms
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Animals
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Cathepsin B / metabolism*
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Dipeptides / chemical synthesis*
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Dipeptides / chemistry
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Dipeptides / metabolism
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Doxorubicin / chemical synthesis*
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Drug Carriers
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Drug Stability
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Humans
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Mitomycin / chemical synthesis*
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Mitomycin / chemistry
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Mitomycin / metabolism
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Paclitaxel / chemical synthesis*
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Paclitaxel / chemistry
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Paclitaxel / metabolism
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Prodrugs / chemical synthesis*
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Prodrugs / chemistry
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Prodrugs / metabolism
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Rats
Substances
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Dipeptides
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Drug Carriers
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Prodrugs
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Mitomycin
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Doxorubicin
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Cathepsin B
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Paclitaxel