In vivo evaluation of P-glycoprotein and breast cancer resistance protein modulation in the brain using [11C]gefitinib

2009 ◽  
Vol 36 (3) ◽  
pp. 239-246 ◽  
Author(s):  
Kazunori Kawamura ◽  
Tomoteru Yamasaki ◽  
Joji Yui ◽  
Akiko Hatori ◽  
Fujiko Konno ◽  
...  
2009 ◽  
Vol 29 (6) ◽  
pp. 1079-1083 ◽  
Author(s):  
Leon M Tai ◽  
A Jane Loughlin ◽  
David K Male ◽  
Ignacio A Romero

The clearance of amyloid beta (Aβ) from the brain represents a novel therapeutic target for Alzheimer's disease. Conflicting data exist regarding the contribution of adenosine triphosphatebinding cassette transporters to the clearance of Aβ through the blood-brain barrier. Therefore, we investigated whether Aβ could be a substrate for P-glycoprotein (P-gp) and/or for breast cancer resistance protein (BCRP) using a human brain endothelial cell line, hCMEC/D3. Inhibition of P-gp and BCRP increased apical-to-basolateral, but not basolateral-to-apical, permeability of hCMEC/D3 cells to 125l Aβ 1–40. Our in vitro data suggest that P-gp and BCRP might act to prevent the blood-borne Aβ 1–40 from entering the brain.


2015 ◽  
Vol 56 (12) ◽  
pp. 1930-1936 ◽  
Author(s):  
A. Traxl ◽  
T. Wanek ◽  
S. Mairinger ◽  
J. Stanek ◽  
T. Filip ◽  
...  

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