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Bioorg Med Chem Lett. 1998 Dec 1;8(23):3341-6.

Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin.

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  • 1Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA.


A series of lysosomal protease-sensitive peptides attached to doxorubicin (DOX) was prepared as model substrates for internalizing anticancer immunoconjugates and potential antimetastasis prodrugs. Rates of cathepsin B-mediated release of free drug was measured for each, and human plasma stabilities for representative examples.

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