The present invention relates to cytostatics which have a tumor-specific action as a result of linkage to specific carbohydrate moeities via preferred linking units which can be selevtively cleaved by enzymes such as metallo matrixproteases (MMPs), elastase or cathepsines, i.e. by enzymes which can especially be found in tumor tissue. The preferred linking units guarantee sufficient serum stability of the conjugate of cytostatic and carbohydrate moeity and, at the same time, the desired intracellular action within tumor cells as a result of its specific enzymatic or hydrolytic cleavability with release of the cytostatic.
本发明涉及细胞毒素,其通过与特定的
碳水化合物结合单元连接,由于这些连接单元可被
金属基质
蛋白酶(MMPs)、
弹性蛋白酶或半胱
氨酸
蛋白酶等酶类选择性地裂解,因此具有肿瘤特异性作用。所述优选的连接单元保证了细胞毒素与
碳水化合物结合物的足够血清稳定性,并且由于其特定的酶促或
水解性裂解而在肿瘤细胞内发挥所需的细胞内作用,从而释放细胞毒素。这些酶类尤其存在于肿瘤组织中。