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

Citation

Velkov, T and Horne, HJ and Laguerre, A and Jones, E and Scanlon, MJ and Porter, CJ, Examination of the role of intestinal fatty acid-binding protein in drug absorption using a parallel artificial membrane permeability assay, Chemistry and Biology, 14, (4) pp. 453-465. ISSN 1074-5521 (2007) [Refereed Article]

DOI: doi:10.1016/j.chembiol.2007.03.009

Abstract

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. © 2007 Elsevier Ltd. All rights reserved.

Item Details

Item Type:Refereed Article
Keywords:fatty acid binding protein drug absorption
Research Division:Biological Sciences
Research Group:Biochemistry and cell biology
Research Field:Structural biology (incl. macromolecular modelling)
Objective Division:Expanding Knowledge
Objective Group:Expanding knowledge
Objective Field:Expanding knowledge in the biological sciences
UTAS Author:Horne, HJ (Dr James Horne)
ID Code:53563
Year Published:2007
Web of Science® Times Cited:30
Deposited By:Central Science Laboratory
Deposited On:2008-12-11
Last Modified:2008-12-11
Downloads:0

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