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

Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels
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DOI:
10.1021/jm991174y
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发表时间:
2000-05-18
影响因子:
7.3
通讯作者:
Karlsson, R
Karlsson, R
中科院分区:
医学1区
文献类型:
--
作者:
Frostell-Karlsson, Å;Remaeus, A;Karlsson, R

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利用表面等离子体共振技术研究了根据报道的人血清白蛋白(HSA)结合水平选择的一组药物与固定化HSA之间的相互作用。固定后主要的HSA结合位点可用。药物与HSA表面相互作用获得的信号强度与报道的HSA结合水平相关。根据药物注射80 μ M浓度将药物分为高、中、低HSA结合组。我们还研究了一组与α(1)-酸性糖蛋白(AGP)结合的10种药物,并与已报道的AGP结合数据进行了关联。该方法的通量为100个化合物/24 h,样品消耗小于100 μ L (8 nmol)。
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).