Effects of Drug Bindings on the Esterase-like Activity of Human Serum Albumin. VII. Subdivision of R-Type Drugs Inhibiting the Activity towards p-Nitrophenyl Acetate(Pharmaceutical)

  • 黒野 幸久
    Faculty of Pharmaceutical Sciences, Nagoya City University
  • 尾関 義郎
    Faculty of Pharmaceutical Sciences, Nagoya City University
  • 山田 秀人
    Faculty of Pharmaceutical Sciences, Nagoya City University
  • 竹内 皮雅
    Faculty of Pharmaceutical Sciences, Nagoya City University
  • 池田 憲
    Faculty of Pharmaceutical Sciences, Nagoya City University

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説明

The subdivision of R-type drugs, which inhibit the reaction of p-nitrophenyl acetate with an active site (R site) located near the tyrosine-411 residue of human serum albumin (HSA), is proposed based on the results of kinetic and fluorometric studies. We found two kinds of R-type drugs with regard to the influence on the reaction rate of 3,5-dinitroaspirin (DA) at a site (U site) near the lysine-199 and tryptophan-214 (Trp-214) residues of HSA. One of them (R_2-type drug, e.g., diazepam or medazepam) greatly accelerates the reaction of DA with HSA, and the other (R_1-type drug, e.g., clofibric acid or octanoic acid) does not affect the reaction. The R_2-type drug quenches the fluorescence originating from the Trp-214 residue in the U site of HSA, and the R_1 type drug hardly influences this fluorescence. The acceleration of the reaction was considered to be due to the conformational change of the U site caused by binding of the R_2-type drug to a part of the R site on HSA. Five benzodiazepines, 3 sulfonylureas, and 3 other drugs were classified into R_1-type and R_2-type drugs.

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