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- W3152308840 abstract "Aim:To develop a complex high-throughput screening (HTS) assay based on scintillation proximity assay (SPA) technology for identification of novel peroxi- some proliferator-activated receptor gamma (PPARγ) modulators.Methods:Full- length PPARγ and retinoid X receptor alpha (RXRα),biotinylated PPAR response element (PPRE),[~3H]BRL49653 and streptavidin-coated FlashPlate or microbead were used to develop an HTS assay based on SPA technology.This‘ABCDE’ method was validated against conventional hydroxyapatite (HA) assay and ap- plied to large-scale screening of 16 000 synthetic compounds and natural product extracts.Results:(1) IC_(50) values of positive control compounds (BRL49653 and troglitazone) obtained from the‘ABCDE’method and HA assay were compa- rable and consistent with those reported elsewhere;(2) Approximately 178 compounds,showing more than 70% competitive inhibition on BRL49653 bind- ing to PPARγ,were identified initially by the‘ABCDE’method (microbead);(3) Secondary screening using FlashPlate and cross-reactivity studies with RARα,β, γ and RXRα,β,γ confirmed that 12 compounds possessed specific PPARγ bind- ing properties including 2 with IC_(50) values less than 0.5 μmol/L and novel chemi- cal structures.Conclusions:The‘ABCDE’method using either FlashPlate or microbead,is a highly efficient,automatable,and robust tool to screen potential PPARγ modulators in HTS setting.Its application may be expanded to other nuclear receptors that form heterodimers upon activation." @default.
- W3152308840 created "2021-04-13" @default.
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- W3152308840 date "2005-01-01" @default.
- W3152308840 modified "2023-09-23" @default.
- W3152308840 title "Development of a complex scintillation proximity assay for highthroughput screening of PPAR7 modulators" @default.
- W3152308840 hasPublicationYear "2005" @default.
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