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| Item Type: | Article |
|---|---|
| Title: | Identification and characterization of a single high-affinity fatty acid binding site in human serum albumin |
| Creators Name: | Wenskowsky, L., Schreuder, H., Derdau, V., Matter, H., Volkmar, J., Nazaré, M., Opatz, T. and Petry, S. |
| Abstract: | A single high-affinity fatty acid binding site in the important human transport protein serum albumin (HSA) is identified and characterized using an NBD (7-nitrobenz-2-oxa-1,3-diazol-4-yl)-C(12) fatty acid. This ligand exhibits a 1:1 binding stoichiometry in its HSA complex with high site-specificity. The complex dissociation constant is determined by titration experiments as well as radioactive equilibrium dialysis. Competition experiments with the known HSA-binding drugs warfarin and ibuprofen confirm the new binding site to be different from Sudlow-sites I and II. These binding studies are extended to other albumin binders and fatty acid derivatives. Furthermore an X-ray crystal structure allows locating the binding site in HSA subdomain IIA. The knowledge about this novel HSA site will be important for drug depot development and for understanding drug-protein interaction, which are important prerequisites for modulation of drug pharmacokinetics. |
| Keywords: | Binding Sites, Drug Interactions, Fatty Acids, Human Serum Albumin, NBD Labels |
| Source: | Angewandte Chemie International Edition |
| ISSN: | 1433-7851 |
| Publisher: | Wiley-VCH |
| Volume: | 57 |
| Number: | 4 |
| Page Range: | 1044-1048 |
| Date: | 22 January 2018 |
| Official Publication: | https://doi.org/10.1002/anie.201710437 |
| PubMed: | View item in PubMed |
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