Albumin microspheres as carrier of an inhibitor of leukocyte elastase: potential therapeutic agent for emphysema.
Albumin microspheres as carrier of an inhibitor of leukocyte elastase: potential therapeutic agent for emphysema.
复制标题
白蛋白微球作为白细胞弹性蛋白酶抑制剂的载体：肺气肿的潜在治疗剂。
DOI：
10.1073/pnas.76.5.2128
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发表时间：
1979
影响因子：
11.1
通讯作者：
G. Krejcarek
中科院分区：
文献类型：
--
作者：
R. R. Martodam;D. Y. Twumasi;I. Liener;J. Powers;N. Nishino;G. Krejcarek
Methods are described for the covalent attachment of succinoyl-Ala-Ala-Pro-ValCH2Cl, an active site-directed inhibitor of human leukocyte elastase (EC 3.4.21.11), to microspheres of human albumin. The insertion of side arms of various lengths revealed that maximum inhibition of this enzyme was obtained when the spacer arm was at least 24.3 A in length. Approximately 30 molecules of the inhibitor could be attached to each molecule of albumin. Such derivatized microspheres were capable of inhibiting approximately one mole of elastase per mole of albumin, which is comparable to the inhibitory activity of alpha 1-antitrypsin. Experiments in vivo in which rats were injected intravenously with radiolabeled microspheres to which the inhibitor had been attached showed a rapid and exclusive uptake by the lungs. About 40--50% of the injected microspheres subsequently remained in the lungs with a half-life of approximately 17 days. These derivatized microspheres thus appear to offer promise as a therapeutic agent for emphysema.
