Characterization of the drug binding specificity of rat liver fatty acid binding protein

Chuang, Sara, Velkov, Tony, Horne, James, Porter, Christopher J. H. and Scanlon, Martin J. 2008, Characterization of the drug binding specificity of rat liver fatty acid binding protein, Journal of medicinal chemistry, vol. 51, no. 13, pp. 3755-3764, doi: 10.1021/jm701192w.

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Title Characterization of the drug binding specificity of rat liver fatty acid binding protein
Author(s) Chuang, Sara
Velkov, Tony
Horne, James
Porter, Christopher J. H.
Scanlon, Martin J.
Journal name Journal of medicinal chemistry
Volume number 51
Issue number 13
Start page 3755
End page 3764
Publisher American Chemical Society
Place of publication Washington, D.C.
Publication date 2008
ISSN 0022-2623
Summary Liver-fatty acid binding protein (L-FABP) is found in high levels in enterocytes and is involved in the cytosolic solubilization of fatty acids during fat absorption. In the current studies, the interaction of L-FABP with a range of lipophilic drugs has been evaluated to explore the potential for L-FABP to provide an analogous function during the absorption of lipophilic drugs. Binding affinity for L-FABP was assessed by displacement of a fluorescent marker, 1-anilinonaphthalene-8-sulfonic acid (ANS), and the binding site location was determined via nuclear magnetic resonance chemical shift perturbation studies. It was found that the majority of drugs bound to L-FABP at two sites, with the internal site generally having a higher affinity for the compounds tested. Furthermore, in contrast to the interaction of L-FABP with fatty acids, it was demonstrated that a terminal carboxylate is not required for specific binding of lipophilic drugs at the internal site of L-FABP.
Language eng
DOI 10.1021/jm701192w
Field of Research 111504 Pharmaceutical Sciences
Socio Economic Objective 970111 Expanding Knowledge in the Medical and Health Sciences
HERDC Research category C1.1 Refereed article in a scholarly journal
ERA Research output type C Journal article
HERDC collection year 2008
Copyright notice ©2008, American Chemical Society
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Document type: Journal Article
Collections: Faculty of Health
School of Medicine
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