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Prodrugs for antibody- and gene-directed enzyme prodrug therapies (ADEPT and GDEPT).

机译:用于抗体和基因指导的酶前药治疗的前药(ADEPT和GDEPT)。

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摘要

Antibody- and gene-directed enzyme prodrug therapy are two-step targeting strategies designed to improve the selectivity of antitumour agents. The approaches are based on the activation of specially designed prodrugs by antibody-enzyme conjugates targeted to tumour-associated antigens (ADEPT) or by enzymes expressed by exogenous genes in tumour cells (GDEPT). Herein the design, synthesis, physico-chemical and biological properties, kinetics and clinical trials of the prodrugs and the enzymes carboxypeptidase G2 and nitroreductase are reviewed for ADEPT and GDEPT.
机译:抗体和基因指导的酶前药治疗是两步靶向策略,旨在提高抗肿瘤药的选择性。这些方法基于专门设计的前药通过靶向肿瘤相关抗原的抗体-酶偶联物(ADEPT)或肿瘤细胞中外源基因表达的酶(GDEPT)的激活。本文对ADEPT和GDEPT的前药和羧肽酶G2和硝基还原酶的设计,合成,理化和生物学性质,动力学和临床试验进行了综述。

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