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Examination of the role of intestinal Fatty acid-binding protein in drug absorption using a parallel artificial membrane permeability assay

Velkov, Tony, Horne, James, Laguerre, Aisha, Jones, Eric, Scanlon, Martin J. and Porter, Christopher J. H. 2007, Examination of the role of intestinal Fatty acid-binding protein in drug absorption using a parallel artificial membrane permeability assay, Chemistry and biology, vol. 14, no. 4, pp. 453-465, doi: 10.1016/j.chembiol.2007.03.009.

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Title Examination of the role of intestinal Fatty acid-binding protein in drug absorption using a parallel artificial membrane permeability assay
Author(s) Velkov, Tony
Horne, James
Laguerre, Aisha
Jones, Eric
Scanlon, Martin J.
Porter, Christopher J. H.
Journal name Chemistry and biology
Volume number 14
Issue number 4
Start page 453
End page 465
Publisher Cell Press
Place of publication Cambridge, Mass.
Publication date 2007-04-20
ISSN 1074-5521
1879-1301
Keyword(s) CHEMBIOL
Summary Transcellular diffusion across the absorptive epithelial cells (enterocytes) of the small intestine is the main route of absorption for most orally administered drugs. The process by which lipophilic compounds transverse the aqueous environment of the cytoplasm, however, remains poorly defined. In the present study, we have identified a structurally diverse group of lipophilic drugs that display low micromolar binding affinities for a cytosolic lipid-binding protein—intestinal fatty acid-binding protein (I-FABP). Binding to I-FABP significantly enhanced the transport of lipophilic drug molecules across a model membrane, and the degree of transport enhancement was related to both drug lipophilicity and I-FABP binding affinity. These data suggest that intracellular lipid-binding proteins such as I-FABP may enhance the membrane transport of lipophilic xenobiotics and facilitate drug access to the enterocyte cytoplasm and cytoplasmic organelles.
Language eng
DOI 10.1016/j.chembiol.2007.03.009
Field of Research 030401 Biologically Active Molecules
060110 Receptors and Membrane Biology
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 ©2007, Elsevier
Persistent URL http://hdl.handle.net/10536/DRO/DU:30019069

Document type: Journal Article
Collection: School of Medicine
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Created: Fri, 11 Sep 2009, 10:28:29 EST by Rachael Wilson

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