Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels

被引:259
作者
Frostell-Karlsson, Å [1 ]
Remaeus, A [1 ]
Roos, H [1 ]
Andersson, K [1 ]
Borg, P [1 ]
Hämäläinen, M [1 ]
Karlsson, R [1 ]
机构
[1] Biacore AB, S-75450 Uppsala, Sweden
关键词
D O I
10.1021/jm991174y
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The interactions between a set of drugs, selected on the basis of reported human serum albumin (HSA) binding levels, and immobilized HSA were investigated using surface plasmon resonance technology. Major HSA binding sites were available after immobilization. The intensity of the signal obtained from the interaction of the drug with the HSA surface was correlated with the reported HSA binding level. Drugs were classified into groups corresponding to high, medium, or low HSA binding based on the injection of the drug at 80 mu M concentration. A set of 10 drugs binding to alpha(1)-acid glycoprotein (AGP) was also investigated and correlated with reported AGP binding data. The throughput of the presented assay is 100 compounds/24 h, and the sample consumption is less than 100 mu L (8 nmol).
引用
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页码:1986 / 1992
页数:7
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