Probing the fibrate binding specificity of rat liver fatty acid binding protein

Chuang, Sara, Velkov, Tony, Horne, James, Wielens, Jerome, Chalmers, David K., Scanlon, Martin J. and Porter, Christopher J. H. 2009, Probing the fibrate binding specificity of rat liver fatty acid binding protein, Journal of medicinal chemistry, vol. 52, no. 17, pp. 5344-5355, doi: 10.1021/jm801349e.

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Title Probing the fibrate binding specificity of rat liver fatty acid binding protein
Author(s) Chuang, Sara
Velkov, Tony
Horne, James
Wielens, Jerome
Chalmers, David K.
Scanlon, Martin J.
Porter, Christopher J. H.
Journal name Journal of medicinal chemistry
Volume number 52
Issue number 17
Start page 5344
End page 5355
Publisher American Chemical Society
Place of publication Washington, D.C.
Publication date 2009-09-10
ISSN 0022-2623
Summary Liver-fatty acid binding protein (L-FABP) is found in high levels in enterocytes and is involved in cytosolic solubilization of fatty acids. In addition, L-FABP has been shown to bind endogenous and exogenous lipophilic compounds, suggesting that it may also play a role in modulating their absorption and disposition within enterocytes. Previously, we have described binding of L-FABP to a range of drugs, including a series of fibrates. In the present study, we have generated structural models of L-FABP-fibrate complexes and undertaken thermodynamic analysis of the binding of fibrates containing either a carboxylic acid or ester functionality. Analysis of the current data reveals that both the location and the energetics of binding are different for fibrates that contain a carboxylate compared to those that do not. As such, the data presented in this study suggest potential mechanisms that underpin molecular recognition and dictate specificity in the interaction between fibrates and L-FABP.
Language eng
DOI 10.1021/jm801349e
Field of Research 030499 Medicinal and Biomolecular Chemistry not elsewhere classified
Socio Economic Objective 970111 Expanding Knowledge in the Medical and Health Sciences
HERDC Research category C1.1 Refereed article in a scholarly journal
Copyright notice ©2009, American Chemical Society
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School of Medicine
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