铂配合物对胰凝乳蛋白酶的影响。

Effects of platinum complexes on chymotrypsin.

作者信息

Melius P, Andersson L A, Lee Y Y

出版信息

J Med Chem. 1980 Jun;23(6):685-7. doi: 10.1021/jm00180a023.

PMID:7190192

Abstract

A variety of platinum complexes were evaluated as inhibitors of alpha-chymotrypsin. A standard enzyme assay was used with benzoyl-L-tyrosine ethyl ester as the substrate. Rb2PtBr4, trans-Pt(NH3)2Cl2, and K2PtCl4 were all effective enzyme inhibitors. Pt(Gly-L-Met(Cl2, Pt(Met)(NH3)2Cl, cis-Pt(NH3)2Cl2, and two ethylenediamminedichloroplatinum complexes were weak inhibitors of alpha-chymotrypsin. A surprising finding was the noninhibition of an immobilized preparation of alpha-chymotrypsin by the above inhibitors and by active-site-directed modifying reagents.

摘要

评估了多种铂配合物作为α-糜蛋白酶抑制剂的效果。采用标准酶分析法，以苯甲酰-L-酪氨酸乙酯作为底物。四溴化铷铂（Rb2PtBr4）、反式二氯二氨合铂（trans-Pt(NH3)2Cl2）和四氯铂酸钾（K2PtCl4）均为有效的酶抑制剂。氯（甘氨酸-L-蛋氨酸）铂（Pt(Gly-L-Met)(Cl2)、氯（蛋氨酸）二氨合铂（Pt(Met)(NH3)2Cl）、顺式二氯二氨合铂（cis-Pt(NH3)2Cl2）以及两种乙二胺二氯铂配合物是α-糜蛋白酶的弱抑制剂。一个惊人的发现是，上述抑制剂以及活性位点定向修饰试剂对固定化的α-糜蛋白酶制剂没有抑制作用。