阿霉素与钙结合位点的相互作用。

Interactions of adriamycin with a calcium binding site.

作者信息

Canada R G, Saway W, Thompson E

机构信息

Department of Physiology and Biophysics, Howard University College of Medicine, Washington, D.C. 20059.

出版信息

Biochem Biophys Res Commun. 1988 Mar 15;151(2):679-85. doi: 10.1016/s0006-291x(88)80334-6.

DOI:10.1016/s0006-291x(88)80334-6

PMID:3348802

Abstract

Terbium (Tb3+) luminescence has been used to investigate the interactions of adriamycin with a specific calcium binding protein, in the plasma membrane of GH3/B6 pituitary tumor cells. The luminescence intensity and lifetime of the Tb3+-GH3/B6 complex was quenched in the presence of adriamycin. According to Stern-Volmer analysis, the quenching of Tb3+-GH3/B6 luminescence was by both membrane bound adriamycin (Ka = 3.7 x 10(5) M-1) and free adriamycin (kq = 7.3 x 10(7) M-1 s-1). The data suggests that, the calcium binding site at the outer surface of the membrane is collisionally accessible to freely diffusing adriamycin; and, that the toxin receptor site is located near the bound metal ion.

摘要

铽（Tb3+）发光已被用于研究阿霉素与生长激素释放激素3/垂体瘤细胞系（GH3/B6）质膜中一种特定钙结合蛋白的相互作用。在阿霉素存在的情况下，Tb3+-GH3/B6复合物的发光强度和寿命会被淬灭。根据斯特恩-沃尔默分析，Tb3+-GH3/B6发光的淬灭是由膜结合阿霉素（Ka = 3.7 x 10(5) M-1）和游离阿霉素（kq = 7.3 x 10(7) M-1 s-1）共同导致的。数据表明，膜外表面的钙结合位点可与自由扩散的阿霉素发生碰撞；并且，毒素受体位点位于结合的金属离子附近。