组织蛋白酶B敏感的二肽前药。1. 阿霉素有效释放的结构要求的模型研究。
Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin.
作者信息
Dubowchik G M, Firestone R A
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA.
出版信息
Bioorg Med Chem Lett. 1998 Dec 1;8(23):3341-6. doi: 10.1016/s0960-894x(98)00609-x.
PMID:9873731
Abstract
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.
摘要
制备了一系列连接阿霉素（DOX）的溶酶体蛋白酶敏感肽，作为内化抗癌免疫缀合物和潜在抗转移前药的模型底物。测定了每种底物中组织蛋白酶B介导的游离药物释放速率，以及代表性实例在人血浆中的稳定性。
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