title: Cathepsin B-sensitive dipeptide prodrugs. 2. Models of anticancer drugs paclitaxel (Taxol), mitomycin C and doxorubicin.
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.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA.
authors.forename: G M
authors.initials: GM
authors.lastname: Dubowchik
authors.forename: K
authors.initials: K
authors.lastname: Mosure
authors.forename: J O
authors.initials: JO
authors.lastname: Knipe
authors.forename: R A
authors.initials: RA
authors.lastname: Firestone
mesh_terms: D000818:Animals; D002401:Cathepsin B / Q000378:metabolism*; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D004317:Doxorubicin / Q000138:chemical synthesis*; D004337:Drug Carriers; D004355:Drug Stability; D006801:Humans; D016685:Mitomycin / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D017239:Paclitaxel / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D011355:Prodrugs / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D051381:Rats
chemical_list: D004151:Dipeptides; D004337:Drug Carriers; D011355:Prodrugs; D016685:Mitomycin; D004317:Doxorubicin; D002401:Cathepsin B; D017239:Paclitaxel