Larionova N I, Mityushina G V, Kazanskaya N F, Blidchenko Y A, Berezin I V
Biol Chem Hoppe Seyler. 1985 Aug;366(8):743-8. doi: 10.1515/bchm3.1985.366.2.743.
The trypsin-kallikrein inhibitor aprotinin was coupled to (carboxymethyl)dextran derivatives of D-galactose. The conjugates contained 14 and 38 D-galactose residues/mol of protein, respectively. The apparent dissociation constants Ki of the complexes between trypsin and modified aprotinins proved to be one order of magnitude higher than the respective values for native aprotinin. The distribution of the modified aprotinins in rat organs after endocardial injection has been studied. The conjugates of aprotinin with (carboxymethyl)dextran derivatives of D-galactose were characterized by decreased clearance rates; they accumulated in the active form in liver. The accumulation was 2.5-10 times higher than native aprotinin for the time of observation (5 min-2 h).
胰蛋白酶 - 激肽释放酶抑制剂抑肽酶与D - 半乳糖的（羧甲基）葡聚糖衍生物偶联。这些缀合物分别含有每摩尔蛋白质14个和38个D - 半乳糖残基。胰蛋白酶与修饰后的抑肽酶之间复合物的表观解离常数Ki被证明比天然抑肽酶的相应值高一个数量级。已经研究了心内膜注射后修饰后的抑肽酶在大鼠器官中的分布。抑肽酶与D - 半乳糖的（羧甲基）葡聚糖衍生物的缀合物的特征在于清除率降低；它们以活性形式在肝脏中积累。在观察时间（5分钟 - 2小时）内，积累量比天然抑肽酶高2.5至10倍。
