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

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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.