Findenig G, Vielnascher E, Göbl R, Fritzer-Szekeres M, Szekeres T
Institut für Medizinische Chemie, Universität Wien.
Wien Klin Wochenschr. 1995;107(22):694-7.
Inhibition of the enzyme ribonucleotide reductase by polyhydroxy-substituted benzohydroxamide derivates is an example for the effects of antimetabolites. We present an overview of the effects of antimetabolites, in particular regarding their action on leukemia cells. Trimidox is one of the most effective inhibitors of ribonucleotide reductase. It inhibits the enzyme in cell extracts as well as in the in situ assay and causes decreased dGTP and dCTP pools in HL-60 cells. We describe combinations with other antimetabolites, as well as biochemical, morphological and cytotoxic effects of trimidox. This manuscript gives an overview of our results with trimidox and describes selection criteria, effects and combinations used in enzyme-targeted chemotherapy.
多羟基取代苯甲羟肟酸衍生物对核糖核苷酸还原酶的抑制作用是抗代谢物作用的一个例子。我们概述了抗代谢物的作用，特别是它们对白血病细胞的作用。三甲曲沙是核糖核苷酸还原酶最有效的抑制剂之一。它在细胞提取物以及原位试验中均能抑制该酶，并导致HL-60细胞中dGTP和dCTP池减少。我们描述了三甲曲沙与其他抗代谢物的联合使用，以及三甲曲沙的生化、形态学和细胞毒性作用。本文概述了我们使用三甲曲沙的研究结果，并描述了酶靶向化疗中使用的选择标准、作用和联合用药。
