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.

نویسندگان

  • Y Kurono
  • Y Ozeki
  • H Yamada
  • T Takeuchi
  • K Ikeda
چکیده

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 (R2-type drug, e.g., diazepam or medazepam) greatly accelerates the reaction of DA with HSA, and the other (R1type drug, e.g., clofibric acid or octanoic acid) does not affect the reaction. The R2-type drug

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عنوان ژورنال:
  • Chemical & pharmaceutical bulletin

دوره 35 2  شماره 

صفحات  -

تاریخ انتشار 1987