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

被引:144
作者
Dubowchik, GM [1 ]
Firestone, RA [1 ]
机构
[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA
关键词
D O I
10.1016/S0960-894X(98)00609-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 1998 Elsevier Science Ltd. All rights reserved.
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页码:3341 / 3346
页数:6
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