scholarly journals Construction of Drug Screening Cell Model and Application to New Compounds Interfering Production and Accumulation of Beta-Amyloid by Inhibiting Gamma-Secretase

Author(s):  
Xiao-Ning Wang ◽  
Jie Yang ◽  
Ping-Yue Xu ◽  
Jie Chen ◽  
Dan Zhang ◽  
...  
2009 ◽  
Vol 76 (1) ◽  
pp. 173-181 ◽  
Author(s):  
H. F. Dovey ◽  
V. John ◽  
J. P. Anderson ◽  
L. Z. Chen ◽  
P. De Saint Andrieu ◽  
...  

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 587 ◽  
Author(s):  
Ina Puscas ◽  
Florian Bernard-Patrzynski ◽  
Martin Jutras ◽  
Marc-André Lécuyer ◽  
Lyne Bourbonnière ◽  
...  

Since most preclinical drug permeability assays across the blood-brain barrier (BBB) are still evaluated in rodents, we compared an in vitro mouse primary endothelial cell model to the mouse b.End3 and the acellular parallel artificial membrane permeability assay (PAMPA) models for drug screening purposes. The mRNA expression of key feature membrane proteins of primary and bEnd.3 mouse brain endothelial cells were compared. Transwell® monolayer models were further characterized in terms of tightness and integrity. The in vitro in vivo correlation (IVIVC) was obtained by the correlation of the in vitro permeability data with log BB values obtained in mice for seven drugs. The mouse primary model showed higher monolayer integrity and levels of mRNA expression of BBB tight junction (TJ) proteins and membrane transporters (MBRT), especially for the efflux transporter Pgp. The IVIVC and drug ranking underlined the superiority of the primary model (r2 = 0.765) when compared to the PAMPA-BBB (r2 = 0.391) and bEnd.3 cell line (r2 = 0.019) models. The primary monolayer mouse model came out as a simple and reliable candidate for the prediction of drug permeability across the BBB. This model encompasses a rapid set-up, a fair reproduction of BBB tissue characteristics, and an accurate drug screening.


2020 ◽  
Vol 14 (2) ◽  
pp. 218-229
Author(s):  
Kattika Kaarj ◽  
Jennifer Ngo ◽  
Christina Loera ◽  
Patarajarin Akarapipad ◽  
Soohee Cho ◽  
...  

Oncotarget ◽  
2015 ◽  
Vol 6 (25) ◽  
pp. 21255-21267 ◽  
Author(s):  
Maria A. Theodoraki ◽  
Celso O. Rezende ◽  
Oraphin Chantarasriwong ◽  
Adriana D. Corben ◽  
Emmanuel A. Theodorakis ◽  
...  

Lab on a Chip ◽  
2014 ◽  
Vol 14 (15) ◽  
pp. 2860-2866 ◽  
Author(s):  
A. Ruiz ◽  
P. Joshi ◽  
R. Mastrangelo ◽  
M. Francolini ◽  
C. Verderio ◽  
...  

Neuronal viability tests performed in primary cultures and co-cultures of the central nervous system grown on microfluidic drug screening chips show a neuroprotective action of FTY720 in cultures degenerated by oligomeric beta amyloid.


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