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[关于在最佳超酸化癌组织中具有激活作用的新型抗癌剂概念的约束矩阵(作者译)]

[Constraints matrix for the concept of new cancerostatics with activation in optimally superacidulated carcinomatous tissue (author's transl)].

作者信息

Ardenne M v, reitnauer P G

出版信息

Arch Geschwulstforsch. 1975;45(1):34-9.

PMID:239667
Abstract

Maintained immunoreaction -- an essential factor for the prospects of healing in any type of cancer therapy -- can be warranted on principle by developing cancerostatics with substantially increased selectivity. One way to approach this goal is the synthesis of functionally masked cancerostatics the active form of which is released only in optimally superacidulated carcinomatous tissue. Used as a key element for such a liberation is a enzyme contained in the cancer cells in its highly concentrated free form. The activity curve of this enzyme must have a pronounced optimum in a span of pH equal 5 to 6. Bonding the active form of, say, an alkylizing molecular group may be glycosidic by nature. Finally, a model is outlined which duly considers the various pharmaco-kinetic aspects.

摘要

维持免疫反应——任何类型癌症治疗中愈合前景的一个关键因素——原则上可以通过开发具有显著提高选择性的抗癌药物来保证。实现这一目标的一种方法是合成功能掩蔽的抗癌药物,其活性形式仅在最佳超酸化的癌组织中释放。癌细胞中以高浓度游离形式存在的一种酶被用作这种释放的关键要素。这种酶的活性曲线在pH值为5至6的范围内必须有一个明显的最佳值。比如说,将烷基化分子基团的活性形式结合可能本质上是糖苷键结合。最后,概述了一个适当考虑各种药代动力学方面的模型。

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