Human drug-binding site

Loo, T. W., Clarke, D. M., Vanadate trapping of nucleotide at the ATP-binding sites of human multidrug resistance P-glycoprotein exposes different residues to the drug-binding site, Proc. Natl. Acad. Sci. USA 2002, 99, 3511-3516. 

Benkestock, K., Edlund, P. O., Roeraade, J. Electrospray ionization mass spectrometry as a tool for determination of drug binding sites to human serum albumin by noncovalent interaction. Rapid Commun Mass Spectrom 2005, 19, 1637-1643. 

Drug distribution in elderly patients may be altered by hypoalbuminemia, qualitative changes in drug-binding sites, reductions in relative muscle mass, increases in the proportion of body fat, and decreases in total body water. The plasma level of free, active drug is often a direct function of the extent of drug binding to plasma proteins. There is a well-documented age-dependent decline (about 20%) in plasma albumin concentration in humans due to a reduced rate of hepatic albumin... 

Characterization of a Major Drug Binding Site in Human Serum Albumin... 

Fehske KJ, Muller WE, Wollert U (1981) The locations of drug binding sites in human serum albumin. Biochemical Pharmacology 30 687-692... 

Muller WE (1989) Drug binding site on human ai-acid glycoprotein. Prog Clin Bio Res 300 363-378... 

G. Sudlow, D.. Birkett, and D. N. Wade, The characterisation of two specific drug binding sites on human serum albumin. Mol. Pharmacol., 11 824 (1975). 

E Brunner and W. E. Muller, Prazosin binding to human aj-add glycoprotein (orosmucoid), human serum albumin, and human serum. Further characterisation of the single drug binding site of orosmucoid, /. Pkarm. Pharmacd.. 37 305 (1985). 

Sjoholm, The specificity of drug binding sites on human serum albumin, Drug-Protein Binding (M. M. Reidenberg and S. Erill, eds,), Praeger, New York, 1986, p. 36. 

Two primary high-affinity drug binding sites for human albumin have been described. Binding site I, initially described for warfarin, was also shown to... 

Fehske KJ, Muller WE. High-affinity binding of ethacrynic acid is mediated by the two most important drug binding sites of human serum albumin. Pharmacology 1986 32(4) 208-13. 

Irikura, M. Takadate, A. Goya, S. Otagiri, M., 7-alkylaminocoumarin-4-acetic acids as fluorescent-probe for studies of drug-binding sites on human serum-albumin, Chem Pharm Bull 1991, 39, 724-728... 

Loo.T.W., Bartlett, M.C.. and Clarke, D.M. (2003) Permanent activation of the human P-glycoprotein by covalent modification of a residue in the drug-binding site. The Journal of Biological Chemistry. 278, 20449-20452. 

Warfarin is specifically bound to drug binding site I (warfarin binding site) on human serum albumin [51], Sudlow et al. [52] evaluated R,S-warfarin,... 

Yamasaki, K. Mamyama, T. Kragh-Hansen, U. Otagiri, M. Characterization of site I on human serum albumin concept about the structure of a drug binding site. Biochim. Biophys. Acta 1996, 1295, 147-157. 

Kim HS, Austin J, and Hage DS (2002) Identifiaction of drug-binding sites on human serum albumin using affinity capillary electrophoresis and chemically modified proteins as buffer additives. Electrophoresis 13 956-963. 

The amount of urate bound in the absence of drugs was regarded as the baseline and the amounts bound in the presence of various drugs were expressed as percentages of the control values (Fig. 2). It can be seen that probenecid, sulfinpyrazone and sodium salicylate all significantly displaced urate from human albumin binding sites, while colchicine had no effect. 

Sulfaphenazole (684) and sulfazamet (685) are both examples of relatively short acting sulfonamides (B-80MI40406) and their antibacterial activity has been tested against Escherichia coli, the former being more effective than the latter. Sulfaphenazole also displaces sulfonyl ureas from protein binding sites on human serum albumin and consequently increases the concentration of the free (active) drug and produces a more intense reaction that may result in hypoglycemia. 

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