Functional Modification of Indole Binding Site with Indomethacin Congeners

Indomethacin and four congeners were shown by equilibrium dialysis to interfere with the binding of L-tryptophan at the primary indole binding site on defatted human serum albumin. Incubation of albumin with l-(p-bromoacetamidobenzoyl)- and l-(m-bromoacetami- dobenzoyl)-5-methoxy-2-methyl-3-indolyla...

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Veröffentlicht in:	Journal of pharmaceutical sciences 1977-07, Vol.66 (7), p.950-955
Hauptverfasser:	Lui, E.M.K., Farmer, P.S., Dean, C.R.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkylation Anti-inflammatory agents-indomethacin and congeners Anti-inflammatory agents—indomethacin and congeners effect on binding of L-tryptophan by defatted human serum albumin Binding Binding protein—L-tryptophan binding by defatted human serum albumin, effect of indomethacin and congeners Binding Sites - drug effects Binding, Competitive - drug effects Chemical Phenomena Chemistry effect of indomethacin and congeners effect on binding of L-tryptophan by defatted human serum albumin functional modification with indomethacin and congeners Humans Indole binding site-on defatted human serum albumin Indole binding site—on defatted human serum albumin functional modification with indomethacin and congeners Indoles - metabolism Indomethacin - analogs & derivatives Indomethacin - pharmacology Indomethacin and congeners-effect on binding of L-tryptophan by defatted human serum albumin Kinetics L-Tryptophan-binding by defatted human serum albumin L-Tryptophan— binding by defatted human serum albumin effect of indomethacin and congeners Protein Binding - drug effects Protein binding-L-tryptophan binding by defatted human serum albumin Protein binding—L-tryptophan binding by defatted human serum albumin effect of indomethacin and congeners protein-L-tryptophan binding by defatted human serum albumin Serum Albumin - metabolism Tryptophan - blood
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Beschreibung
Zusammenfassung:	Indomethacin and four congeners were shown by equilibrium dialysis to interfere with the binding of L-tryptophan at the primary indole binding site on defatted human serum albumin. Incubation of albumin with l-(p-bromoacetamidobenzoyl)- and l-(m-bromoacetami- dobenzoyl)-5-methoxy-2-methyl-3-indolylacetic acids functionally modified this site, decreasing the availability of the site for the binding of L-tryptophan. Incubation in the presence of a large excess of L- tryptophan resulted in the partial protection of the site from modification by 1-(m -bromoacetamidobenzoyl) -5-methoxy-2-methyl-3-indolylacetic acid.
ISSN:	0022-3549 1520-6017
DOI:	10.1002/jps.2600660712