Faculty Opinions recommendation of Coordinated nuclear receptor regulation of the efflux transporter, Mrp2, and the phase-II metabolizing enzyme, GSTpi, at the blood-brain barrier.

2016 ◽  
Author(s):  
Norman Saunders
Keyword(s):  
Blood Brain Barrier ◽  
Nuclear Receptor ◽  
Phase Ii ◽  
Brain Barrier ◽  
Receptor Regulation ◽  
Efflux Transporter ◽  
Blood Brain ◽  
Metabolizing Enzyme

scholarly journals Coordinated Nuclear Receptor Regulation of the Efflux Transporter, Mrp2, and the Phase-Ii Metabolizing Enzyme, GSTπ, at the Blood—Brain Barrier

2008 ◽  
Vol 28 (6) ◽  
pp. 1222-1234 ◽  
Author(s):  
Björn Bauer ◽  
Anika M S Hartz ◽  
Jonathan R Lucking ◽  
Xiaodong Yang ◽  
Gary M Pollack ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Nuclear Receptor ◽  
Brain Barrier ◽  
Efflux Transporter ◽  
Transport Activity ◽  
Brain Capillaries ◽  
Blood Brain ◽  
Metabolizing Enzyme

Xenobiotic efflux pumps at the blood—brain barrier are critical modulators of central nervous system pharmacotherapy. We previously found expression of the ligand-activated nuclear receptor, pregnane X receptor (PXR), in rat brain capillaries, and showed increased expression and transport activity of the drug efflux transporter, P-glycoprotein, in capillaries exposed to PXR ligands (pregnenolone-16α-carbonitrile (PCN) and dexamethasone) in vitro and in vivo. Here, we show increased protein expression and transport activity of another efflux pump, multidrug resistance-associated protein isoform 2 (Mrp2), in rat brain capillaries after in vitro and in vivo exposure to PCN and dexamethasone. The phase-II drug-metabolizing enzyme, glutathione S-transferase-π (GSTπ), was found to be expressed in brain capillaries, where it colocalized to a large extent with Mrp2 at the endothelial cell luminal plasma membrane. Like Mrp2, GSTπ protein expression increased with PXR activation. Colocalization and coordinated upregulation suggest functional coupling of the metabolizing enzyme and efflux transporter. These findings indicate that, as in hepatocytes, brain capillaries possess a regulatory network consisting of nuclear receptors, metabolizing enzymes, and efflux transporters, which modulate blood—brain barrier function.

scholarly journals Amyloid Efflux Transporter Expression at the Blood-Brain Barrier Declines in Normal Aging

2010 ◽  
Vol 69 (10) ◽  
pp. 1034-1043 ◽  
Author(s):  
Gerald D. Silverberg ◽  
Arthur A. Messier ◽  
Miles C. Miller ◽  
Jason T. Machan ◽  
Samir S. Majmudar ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Normal Aging ◽  
Brain Barrier ◽  
Efflux Transporter ◽  
Blood Brain ◽  
Transporter Expression

scholarly journals [11C]Flumazenil brain uptake is influenced by the blood-brain barrier efflux transporter P-glycoprotein

2012 ◽  
Vol 2 (1) ◽  
pp. 12 ◽  
Author(s):  
Femke E Froklage ◽  
Stina Syvänen ◽  
N Harry Hendrikse ◽  
Marc C Huisman ◽  
Carla FM Molthoff ◽  
...  
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Brain Uptake ◽  
Efflux Transporter ◽  
P Glycoprotein ◽  
Blood Brain

Expression of nuclear receptor mRNA and liver X receptor-mediated regulation of ABC transporter A1 at rat blood–brain barrier

2008 ◽  
Vol 52 (4-5) ◽  
pp. 669-674 ◽  
Author(s):  
Shin-ichi Akanuma ◽  
Satoko Hori ◽  
Sumio Ohtsuki ◽  
Masachika Fujiyoshi ◽  
Tetsuya Terasaki
Keyword(s):  
Blood Brain Barrier ◽  
Nuclear Receptor ◽  
Abc Transporter ◽  
Liver X Receptor ◽  
Brain Barrier ◽  
Rat Blood ◽  
Receptor Mrna ◽  
Blood Brain

P4-176: Activity of P-glycoprotein, an ABC efflux transporter at the blood-brain barrier, is compromised in Alzheimer's disease

2012 ◽  
Vol 8 (4S_Part_19) ◽  
pp. P698-P698
Author(s):  
Anand Deo ◽  
Soo Borson ◽  
Jeanne Link ◽  
Janet Eary ◽  
Todd Richards ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Efflux Transporter ◽  
P Glycoprotein ◽  
Blood Brain
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