Niculescu-Duvaz I, Friedlos F, Niculescu-Duvaz D, Davies L, Springer C J
CRC Centre for Cancer Therapeutics at the Institute of Cancer Research, Sutton, Surrey, UK.
Anticancer Drug Des. 1999 Dec;14(6):517-38.
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.
抗体导向酶前药疗法和基因导向酶前药疗法是旨在提高抗肿瘤药物选择性的两步靶向策略。这些方法基于通过靶向肿瘤相关抗原的抗体 - 酶偶联物（抗体导向酶前药疗法）或肿瘤细胞中外源基因表达的酶（基因导向酶前药疗法）激活特殊设计的前药。本文综述了用于抗体导向酶前药疗法和基因导向酶前药疗法的前药以及羧肽酶G2和硝基还原酶的设计、合成、物理化学和生物学性质、动力学及临床试验。
