组织蛋白酶B敏感的二肽前药。2. 抗癌药物紫杉醇（泰素）、丝裂霉素C和阿霉素的模型。
Cathepsin B-sensitive dipeptide prodrugs. 2. Models of anticancer drugs paclitaxel (Taxol), mitomycin C and doxorubicin.
作者信息
Dubowchik G M, Mosure K, Knipe J O, 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):3347-52. doi: 10.1016/s0960-894x(98)00610-6.
PMID:9873732
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.
摘要
制备了通过自裂解间隔基与组织蛋白酶B敏感二肽苯丙氨酸-赖氨酸相连的含有阿霉素（DOX）、紫杉醇（紫杉醇）和丝裂霉素C（MMC）的底物，作为内化抗癌免疫缀合物的模型化合物。分别测定了组织蛋白酶B介导的游离药物释放速率、大鼠肝脏溶酶体敏感性和人血浆稳定性。
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