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Title 

A simple method to screen ligands of peroxisome proliferator-activated receptor δ

Authors 

M C ChoH E YoonJ W KangS W ParkY YangJ T HongEun Young SongS G PaikS H KimD Y Yoon

Publisher 

Elsevier

Issue Date 

2006

Citation 

European Journal of Pharmaceutical Sciences, vol. 29, no. 5, pp. 355-360

Keywords 

co-activatorELISAmetabolic disordersPPARδPPARδ ligandskin disordersligandlinoleic acidnuclear receptor coactivator 2peroxisome proliferator activated receptor delta

Abstract 

Peroxisome proliferator-activated receptors (PPARs) are transcription factors that belong to the nuclear receptor superfamily directly modulating gene expression by binding to specific ligands. Recently, it has been reported that PPARδ ligands play an essential role in improvement of metabolic disorders and skin disorders. We introduce an enzyme-linked immunosorbent assay (ELISA) to screen new PPARδ ligands. This method is based on the activation mechanism of PPARδ where the ligand binding to PPARδ induces the interaction of the receptor with transcriptional co-activators. We optimized a simple ELISA method for screening PPARδ ligands. Among co-activators such as SRC-1, TIF-2, and p300, PPARδ had more strong binding with SRC-1 in an ELISA system. GW501516 and linoleic acid, the well-known ligands of PPARδ, increased the binding between PPARδ and co-activators in a ligand dose-dependent manner. The recruitment of co-activator SRC-1 was also more effective than those of TIF-2 and p300. We optimized and developed a novel and useful ELISA system for the mass screening of PPARδ ligands. This screening system may be useful in the development of drugs for metabolic disorders and skin disorders.

ISSN 

0928-0987

Link 

http://dx.doi.org/10.1016/j.ejps.2006.07.003

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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