Binding of ketoprofen to human serum albumin studied by circular dichroism. 1994

V Russeva, and R Rakovska, and N Stavreva, and D Mihailova, and N Berova
Department of Chemistry, Faculty of Pharmacy, Bulgarian Academy of Sciences, Sofia.

The protein binding of ketoprofen has been studied using circular dichroism titration method as well as the new algorithm proposed by the authors for the treatment of data obtained. The quantitative parameters association constants (k) and number of binding sites (N) have been determined. It is proved that the protein binding of Ketoprofen is going through separate stages and the number of binding sites probably arises. It is acceptable that a high affinity binding takes place primarily (kI = 3.8 x 10(6) l.mol-1). Later, due to the conformational changes in the protein molecule the binding areas are modified and the number of binding sites considerably arises (NI = 3.5 and NII = 14), while the binding affinity reduces 100-fold (kII = 5.10(4) l.mol-1). The number of binding sites has been studied and an identification of the chromophore taking part in the drug-protein interaction has been performed on the base of UV- and CD spectra. A mechanism of the interaction is proposed which coincides with the stepwise binding model.

UI MeSH Term Description Entries
D007660 Ketoprofen An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It is used in the treatment of rheumatoid arthritis and osteoarthritis. Benzoylhydratropic Acid,19,583 RP,2-(3-Benzoylphenyl)propionic Acid,Alrheumat,Alrheumum,Orudis,Profenid,RP-19583,RP 19583,RP, 19,583,RP19583
D008956 Models, Chemical Theoretical representations that simulate the behavior or activity of chemical processes or phenomena; includes the use of mathematical equations, computers, and other electronic equipment. Chemical Models,Chemical Model,Model, Chemical
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D002942 Circular Dichroism A change from planar to elliptic polarization when an initially plane-polarized light wave traverses an optically active medium. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Circular Dichroism, Vibrational,Dichroism, Circular,Vibrational Circular Dichroism
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D012709 Serum Albumin A major protein in the BLOOD. It is important in maintaining the colloidal osmotic pressure and transporting large organic molecules. Plasma Albumin,Albumin, Serum
D013056 Spectrophotometry, Ultraviolet Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Ultraviolet Spectrophotometry

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