文章基本信息

标题：Characterization of a Binding Site of UCN-01, a Novel Anticancer Drug on α1-Acid Glycoprotein
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作者：Noriaki KURATA ; Sadaharu MATSUSHITA ; Koji NISHI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：7
页码：893-895
DOI：10.1248/bpb.23.893
出版社：The Pharmaceutical Society of Japan
摘要：The binding site of 7-hydroxystaurosporine (UCN-01) on α₁-acid glycoprotein (AGP) was studied by fluorescence and ultracentrifugation experiments. Three ligands, propranolol, warfarin and progesterone were employed as marker ligands and quinaldine red was employed as a fluorescent probe. The persence of UCN-01, propranolol, warfarin and progesterone resulted in a significant quenching of the fluorescence of quinaldine red, when bound to AGP, depending upon the potency of the binding to AGP. The construction of Klotz plots indicated that the displacement effects of propranolol, warfarin and progesterone on UCN-01-AGP binding were competitive in nature. These data suggest that the binding site of UCN-01 on the AGP partly overlaps and binding site for basic drugs, acidic drugs, as well as steroid hormones.
关键词：UCN-01;α1-acid glycoprotein;binding site;competitive displacement