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Development of a High-Throughput Assay for Screening of γ-Secretase Inhibitor with Endogenous Human, Mouse or Drosophila γ-Secretase

by Lie-Feng Wang 1, Ru Zhang 1 and Xin Xie 1,2,*
1
Laboratory of Receptor-based Bio-medicine, School of Life Sciences and Technology, Tongji University, Shanghai 200092, China
2
State Key Laboratory of Drug Research, The National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
*
Author to whom correspondence should be addressed.
Molecules 2009, 14(9), 3589-3599; https://doi.org/10.3390/molecules14093589
Received: 30 July 2009 / Revised: 22 August 2009 / Accepted: 31 August 2009 / Published: 14 September 2009
Selective lowering of amyloid-β levels with small-molecule γ-secretase inhibitors is a promising therapeutic approach for Alzheimer’s disease. In this work, we developed a high throughput assay for screening of γ-secretase inhibitors with endogenous γ-secretase and a fluorogenic substrate. The IC50 values of known γ-secretase inhibitors generated with this method were comparable with reported values obtained by other methods. The assay was optimized and applied to a small-scale screening of 1,280 compounds. The discovery of several new inhibitors warrants further investigation. This assay was also proven to be easily adopted to test compounds for drosophila and mouse γ-secretase, which could be very useful to assess compounds activity against γ-secretase from different species before the in vivo test in animal models. View Full-Text
Keywords: γ-secretase inhibitor; fluorogenic substrate; high throughput screening γ-secretase inhibitor; fluorogenic substrate; high throughput screening
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Wang, L.-F.; Zhang, R.; Xie, X. Development of a High-Throughput Assay for Screening of γ-Secretase Inhibitor with Endogenous Human, Mouse or Drosophila γ-Secretase. Molecules 2009, 14, 3589-3599.

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