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Interactions between Human Liver Fatty Acid Binding Protein and Peroxisome Proliferator Activated Receptor Selective Drugs
Author
Source
Issue
Vol. 2013, Issue 2013 (31 Dec. 2013), pp.1-14, 14 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2013-02-18
Country of Publication
Egypt
No. of Pages
14
Main Subjects
Natural & Life Sciences (Multidisciplinary)
Biology
Abstract EN
Fatty acid binding proteins (FABPs) act as intracellular shuttles for fatty acids as well as lipophilic xenobiotics to the nucleus, where these ligands are released to a group of nuclear receptors called the peroxisome proliferator activated receptors (PPARs).
PPAR mediated gene activation is ultimately involved in maintenance of cellular homeostasis through the transcriptional regulation of metabolic enzymes and transporters that target the activating ligand.
Here we show that liver- (L-) FABP displays a high binding affinity for PPAR subtype selective drugs.
NMR chemical shift perturbation mapping and proteolytic protection experiments show that the binding of the PPAR subtype selective drugs produces conformational changes that stabilize the portal region of L-FABP.
NMR chemical shift perturbation studies also revealed that L-FABP can form a complex with the PPAR ligand binding domain (LBD) of PPARα.
This protein-protein interaction may represent a mechanism for facilitating the activation of PPAR transcriptional activity via the direct channeling of ligands between the binding pocket of L-FABP and the PPARαLBD.
The role of L-FABP in the delivery of ligands directly to PPARα via this channeling mechanism has important implications for regulatory pathways that mediate xenobiotic responses and host protection in tissues such as the small intestine and the liver where L-FABP is highly expressed.
American Psychological Association (APA)
Velkov, Tony. 2013. Interactions between Human Liver Fatty Acid Binding Protein and Peroxisome Proliferator Activated Receptor Selective Drugs. PPAR Research،Vol. 2013, no. 2013, pp.1-14.
https://search.emarefa.net/detail/BIM-509752
Modern Language Association (MLA)
Velkov, Tony. Interactions between Human Liver Fatty Acid Binding Protein and Peroxisome Proliferator Activated Receptor Selective Drugs. PPAR Research No. 2013 (2013), pp.1-14.
https://search.emarefa.net/detail/BIM-509752
American Medical Association (AMA)
Velkov, Tony. Interactions between Human Liver Fatty Acid Binding Protein and Peroxisome Proliferator Activated Receptor Selective Drugs. PPAR Research. 2013. Vol. 2013, no. 2013, pp.1-14.
https://search.emarefa.net/detail/BIM-509752
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-509752