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骨髓移植疗效主要受预处理方案限制,而预处理方案中又以烷化荆为主,因此提高烷化剂疗效可望影响预处理方案的效果及其治愈的可能性。调节剂本身通常是一种无毒性、但能调节药物化学药理的某个方面从而提高疗效的化合物。本文扼要地介绍了烷化剂的调节剂。细胞膜有些烷化剂,尤其是氮芥和苯丙酸氮芥是主动转运进入细胞浆的。对这些药物耐药的细胞系其转运减少。氮芥和苯丙酸氮芥的正常底物分别为胆碱和苯丙酸。这两个底物能与各自烷化剂竞争细胞膜的转运,从而减低其细胞毒性。但迄今尚无临床前的实验证明该疗法的优点。
The efficacy of bone marrow transplantation is mainly limited by the pretreatment plan, and the alkylation agent is the main pretreatment protocol. Therefore, improving the effectiveness of the alkylating agent may affect the effectiveness of the preconditioning program and the possibility of its cure. The modulator itself is usually a compound that is non-toxic, but that can regulate certain aspects of the pharmaceutical chemistry to improve efficacy. This article briefly introduces the alkylating agent regulators. Some of the cell membrane alkylating agents, especially nitrogen mustard and phenylalrine mustard, are actively transported into the cytoplasm. The drug resistance of these drug-resistant cell lines is reduced. The normal substrates for nitrogen mustard and phenylpropionic acid mustard were choline and phenylproprionic acid, respectively. These two substrates can compete with their respective alkylating agents for transport of cell membranes, thereby reducing their cytotoxicity. However, no preclinical experiments have so far demonstrated the advantages of this therapy.