Reversible binding of ethacrynic acid to human serum albumin: Difference circular dichroism study

The reversible binding of ethacrynic acid was characterized by a difference circular dichroism method. A 2/1 stoichiometry was determined for the [drug]/[HSA] (human serum albumin) complex. The reversible binding of ethacrynic acid to HSA determines direct competition with ligands that selectivity b...

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Veröffentlicht in:	Chirality (New York, N.Y.) N.Y.), 1999, Vol.11 (1), p.33-38
Hauptverfasser:	Bertucci, Carlo, Nanni, Barbara, Salvadori, Piero
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Anxiety Agents - blood Anti-Anxiety Agents - metabolism Anti-Inflammatory Agents, Non-Steroidal - blood Anti-Inflammatory Agents, Non-Steroidal - metabolism Bilirubin - metabolism Binding Sites Binding, Competitive - drug effects Biomarkers Circular Dichroism cys34 modified albumin Diazepam - blood Diazepam - metabolism Diuretics - blood Diuretics - metabolism ethacrynic acid Ethacrynic Acid - blood Ethacrynic Acid - metabolism HSA binding Humans interaction between drugs Phenylbutazone - blood Phenylbutazone - metabolism Protein Binding Serum Albumin - metabolism stereoselectivity
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Zusammenfassung:	The reversible binding of ethacrynic acid was characterized by a difference circular dichroism method. A 2/1 stoichiometry was determined for the [drug]/[HSA] (human serum albumin) complex. The reversible binding of ethacrynic acid to HSA determines direct competition with ligands that selectivity bind to site II and to the fatty acid site. Furthermore, indirect competition was shown for ligands for site I (anticooperative) and to site III (cooperative). Chirality 11:33–38, 1999. © 1999 Wiley‐Liss, Inc.
ISSN:	0899-0042 1520-636X
DOI:	10.1002/(SICI)1520-636X(1999)11:1<33::AID-CHIR6>3.0.CO;2-U