Analysis of free fatty acid effect on methotrexate binding to albumin. 1994

P Claudepierre, and S Urien, and O Chassany, and J P Tillement
Laboratoire de Pharmacologie, Faculté de Médecine, Université Paris XII, France.

The binding of methotrexate to human serum albumin and the inhibitory effect of serum free fatty acids (FFA) have been studied by equilibrium dialysis with radiolabeled methotrexate. Methotrexate was bound to albumin via a single site (1.03 +/- 0.02) with a low affinity (1350 +/- 60 M-1). The effect of FFA on binding by albumin of methotrexate was analysed according to the classical inhibition models with computation of the free inhibitor concentration and was ascribed to an uncompetitive type of inhibition. These results were in agreement with the observed serum binding of methotrexate (45-50%) and allowed the simulation of the effect of various concentrations of FFA on methotrexate albumin binding in human serum.

UI MeSH Term Description Entries
D008433 Mathematics The deductive study of shape, quantity, and dependence. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed) Mathematic
D008727 Methotrexate An antineoplastic antimetabolite with immunosuppressant properties. It is an inhibitor of TETRAHYDROFOLATE DEHYDROGENASE and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA. Amethopterin,Methotrexate Hydrate,Methotrexate Sodium,Methotrexate, (D)-Isomer,Methotrexate, (DL)-Isomer,Methotrexate, Dicesium Salt,Methotrexate, Disodium Salt,Methotrexate, Sodium Salt,Mexate,Dicesium Salt Methotrexate,Hydrate, Methotrexate,Sodium, Methotrexate
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
D005230 Fatty Acids, Nonesterified FATTY ACIDS found in the plasma that are complexed with SERUM ALBUMIN for transport. These fatty acids are not in glycerol ester form. Fatty Acids, Free,Free Fatty Acid,Free Fatty Acids,NEFA,Acid, Free Fatty,Acids, Free Fatty,Acids, Nonesterified Fatty,Fatty Acid, Free,Nonesterified Fatty Acids
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
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

Related Publications

P Claudepierre, and S Urien, and O Chassany, and J P Tillement
January 1981, Pharmacology,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
January 1980, Acta pharmaceutica Suecica,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
November 1973, Annals of the New York Academy of Sciences,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
May 1991, International journal of clinical pharmacology, therapy, and toxicology,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
May 1975, Journal of lipid research,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
March 1972, Biochimica et biophysica acta,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
July 1980, The Journal of biological chemistry,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
August 1971, Biochemistry,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
June 2014, Physical chemistry chemical physics : PCCP,
P Claudepierre, and S Urien, and O Chassany, and J P Tillement
February 1972, The Biochemical journal,
Copied contents to your clipboard!