The Effect of Bcrp1 (Abcg2) on the In vivo Pharmacokinetics and Brain Penetration of Imatinib Mesylate (Gleevec): Implications for the Use of Breast Cancer Resistance Protein and P-Glycoprotein Inhibitors to Enable the Brain Penetration of Imatinib in Patients

2005 ◽  
Vol 65 (7) ◽  
pp. 2577-2582 ◽  
Author(s):  
Pauline Breedveld ◽  
Dick Pluim ◽  
Greta Cipriani ◽  
Peter Wielinga ◽  
Olaf van Tellingen ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Resistance Protein ◽  
Cancer Resistance ◽  
Brain Penetration ◽  
P Glycoprotein ◽  
Resistance Protein ◽  
Glycoprotein Inhibitors ◽  
The Brain ◽  
In Vivo Pharmacokinetics

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 ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Resistance Protein ◽  
Cancer Resistance ◽  
In Vivo Evaluation ◽  
P Glycoprotein ◽  
Resistance Protein ◽  
The Brain

P-glycoprotein and breast cancer resistance protein restrict the brain penetration of the CDK4/6 inhibitor palbociclib

2015 ◽  
Vol 33 (5) ◽  
pp. 1012-1019 ◽  
Author(s):  
Mark C. de Gooijer ◽  
Ping Zhang ◽  
Nishita Thota ◽  
Isabel Mayayo-Peralta ◽  
Levi C. M. Buil ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Breast Cancer Resistance Protein ◽  
Cancer Resistance ◽  
Brain Penetration ◽  
P Glycoprotein ◽  
Resistance Protein ◽  
The Brain

scholarly journals P-Glycoprotein and Breast Cancer Resistance Protein Restrict Apical-to-Basolateral Permeability of Human Brain Endothelium to Amyloid-β

2009 ◽  
Vol 29 (6) ◽  
pp. 1079-1083 ◽  
Author(s):  
Leon M Tai ◽  
A Jane Loughlin ◽  
David K Male ◽  
Ignacio A Romero
Keyword(s):  
Breast Cancer ◽  
Human Brain ◽  
Breast Cancer Resistance Protein ◽  
Amyloid Β ◽  
Cancer Resistance ◽  
Glycoprotein P ◽  
P Glycoprotein ◽  
Resistance Protein ◽  
The Brain

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.

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