Kraker A, Schmidt J, Krezoski S, Petering D H
Biochem Biophys Res Commun. 1985 Jul 31;130(2):786-92. doi: 10.1016/0006-291x(85)90485-1.
The antitumor agent, cis-dichlorodiammine Pt(II), is cytotoxic to Ehrlich cells in culture. These cells contain a substantial amount of metallothionein in the absence of inducers of the protein. At concentrations of drug which cause 60% inhibition of cell proliferation, most of the platinum is found in the cytosol. Of this about 30% is bound in the metallothionein fraction. Isolated rat liver metallothionein reacts slowly with hydrolyzed cis-dichlorodiammine Pt(II). Thus, metallothionein is a major cellular site of binding of the platinum complex at concentrations which inhibit tumor growth.
抗肿瘤药物顺二氯二氨合铂（II）对培养中的艾氏腹水癌细胞具有细胞毒性。这些细胞在没有该蛋白诱导剂的情况下含有大量金属硫蛋白。在导致细胞增殖受到60%抑制的药物浓度下，大部分铂存在于细胞溶质中。其中约30%与金属硫蛋白部分结合。分离出的大鼠肝脏金属硫蛋白与水解后的顺二氯二氨合铂（II）反应缓慢。因此，在抑制肿瘤生长的浓度下，金属硫蛋白是铂配合物的主要细胞结合位点。
