scholarly journals Small Molecule Amyloid-β Protein Precursor Processing Modulators Lower Amyloid-β Peptide Levels via cKit Signaling

2019 ◽  
Vol 67 (3) ◽  
pp. 1089-1106 ◽  
Author(s):  
Ci-Di Chen ◽  
Ella Zeldich ◽  
Christina Khodr ◽  
Kaddy Camara ◽  
Tze Yu Tung ◽  
...  
2005 ◽  
Vol 10 (1) ◽  
pp. 1-12 ◽  
Author(s):  
Pancham Bakshi ◽  
Yung-Feng Liao ◽  
Jun Gao ◽  
Jake Ni ◽  
Ross Stein ◽  
...  

Cerebral accumulation of the amyloid β-peptide (Aβ) is believed to play a key role in the pathogenesis of Alzheimer’s disease (AD). Because Aβ is produced from the proteolysis of amyloid β-protein precursor (APP) by β-and γ-secretases, these enzymes are considered important drug targets for AD. The authors have developed a luciferase-based reporter system that can identify new molecules that inhibit APP processing in a high-throughput manner. Such molecules can help in understanding the biology of APP and APP processing and in developing new drug prototypes for AD. In this system, APP is fused on its C-terminus with Gal4-VP16, a chimeric yeast-viral transcription activator, and luciferase is under control of the yeast Gal4 promoter. Compounds that modulate the luciferase signal may affect the secretases directly, interact with modifiers of these proteases, or interact with APP directly. The authors successfully interfaced this assay with a high-throughput screen, testing ~60,000 compounds with diverse chemical structures. In principle, this sensitive, specific, and quantitative assay may be useful for identifying both inhibitors and stimulators of APP processing.( Journal of Biomolecular Screening 2005:1-12)


2011 ◽  
Vol 23 (3) ◽  
pp. 521-535 ◽  
Author(s):  
Luis De Taboada ◽  
Jin Yu ◽  
Salim El-Amouri ◽  
Sebastiano Gattoni-Celli ◽  
Steve Richieri ◽  
...  

2005 ◽  
Vol 7 (2) ◽  
pp. 139-148 ◽  
Author(s):  
Xiao-Ping Shi ◽  
Katherine Tugusheva ◽  
James E. Bruce ◽  
Adam Lucka ◽  
Elizabeth Chen-Dodson ◽  
...  

2009 ◽  
Vol 21 (4) ◽  
pp. 567-576 ◽  
Author(s):  
Michael A. Myre ◽  
Kevin Washicosky ◽  
Robert D. Moir ◽  
Giuseppina Tesco ◽  
Rudolph E. Tanzi ◽  
...  

2002 ◽  
Vol 4 (5) ◽  
pp. 405-415 ◽  
Author(s):  
Tadanobu Utsuki ◽  
Mohammed Shoaib ◽  
Harold W. Holloway ◽  
Donald K. Ingram ◽  
William C. Wallace ◽  
...  

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