Microenviromental Analysis of Drug Binding Site on Albumin by Point-mutation and Using Probe

众所周知，人血清白蛋白（HSA）具有3个药物特异性结合位点，分别为位点I、位点II和位点III，近年来的X射线晶体分析表明，主要的药物结合位点位于IIA和IIIA亚区，但大鼠、兔和狗等实验动物血清白蛋白的药物结合位点尚未确定。因此，本研究旨在研究上述动物中这些药物结合位点的表征。所有的白蛋白检测发现至少有两个特异性药物结合位点类似于人白蛋白使用荧光探针。此外，使用不同的结合模型假设独立，竞争和反合作的结合，这些假设得到了支持。白蛋白分子上的位点I或位点II似乎是由亚位点组成的宽区域。然而，不幸的是，我们不能确定微环境分析使用点诱变技术。

It is well-known that human serum albumin (HSA) has three specific binding sites for drugs, called site I,site II and site III.In addition, recent studies by X-ray crystal analysis indicated that the principal drug binding sites are located in subdomains IIA and IIIA.However, the drug binding sites on serum albumin for experimental animals such as rat, rabbit and dog have not yet been determined. Therefore, this investigation has been undertaken to study the characterization of these drug binding sites in the abovementioned animals. All the albumin examined have found to have at least two specific drug binding sites similar to human albumin using fluorescent probes. Further, using the different binding models assuming independent, competitive and anticooperative binding, these hypothesis were supported. The site I or site II on the albumin molecules seemed to be wide area consisting of subsites. However, unfortunately, we could not determine the microenvironmental analysis using the point-mutagenic techniques.