Characterization of lipophilic drug binding to rat intestinal fatty acid binding protein

Velkov, Tony, Lim, Maria L. R., Horne, James, Simpson, Jamie S., Porter, Christopher J. H. and Scanlon, Martin J. 2009, Characterization of lipophilic drug binding to rat intestinal fatty acid binding protein, Molecular and cellular biochemistry, vol. 326, no. 1-2, pp. 87-95, doi: 10.1007/s11010-008-0009-x.

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Title Characterization of lipophilic drug binding to rat intestinal fatty acid binding protein
Author(s) Velkov, Tony
Lim, Maria L. R.
Horne, James
Simpson, Jamie S.
Porter, Christopher J. H.
Scanlon, Martin J.
Journal name Molecular and cellular biochemistry
Volume number 326
Issue number 1-2
Start page 87
End page 95
Publisher Kluwer Academic Publishers
Place of publication New York, N.Y.
Publication date 2009-06
ISSN 0300-8177
Keyword(s) intestinal drug absorption
drug transport
intestinal fatty acid binding protein
fluorescence-based thermal-shift assay
Summary Intestinal fatty acid binding protein (I-FABP) is present at high levels in the absorptive cells of the intestine (enterocytes) where it plays a role in the intracellular solubilization of fatty acids (FA). However, I-FABP has also been shown to bind to a range of non-FA ligands, including some lipophilic drug molecules, albeit with generally lower affinity than FA. The significance of these lower affinity interactions with exogenous compounds is not known. In this manuscript, we describe further characterization of drug-rat I-FABP binding interactions using a thermal-shift assay. A structural explanation of the observed affinity of rat I-FABP for different drugs based on spectroscopic data and modeling experiments is presented. In addition, immunocytochemistry has been used to probe the expression of I-FABP in a cell culture model reflective of the absorptive cells of the small intestine. Taken together, these data suggest a possible role for I-FABP in the disposition of some lipophilic drugs within the enterocyte.
Language eng
DOI 10.1007/s11010-008-0009-x
Field of Research 110601 Biomechanics
Socio Economic Objective 970111 Expanding Knowledge in the Medical and Health Sciences
HERDC Research category C1.1 Refereed article in a scholarly journal
HERDC collection year 2009
Copyright notice ©2009, Springer Science+Business Media, LLC
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Document type: Journal Article
Collections: Faculty of Health
School of Medicine
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