Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2003-4-11
pubmed:abstractText
Peroxisome proliferator-activated receptors (PPARs) are orphan nuclear hormone receptors that are known to control the expression of genes that are involved in lipid homeostasis and energy balance. PPARs activate gene transcription in response to a variety of compounds, including hypolipidemic drugs. Most of these compounds have high affinity to the ligand-binding domain (LBD) of PPARs and cause a conformational change within PPARs. As a result, the receptor is converted to an activated mode that promotes the recruitment of co-activators such as the steroid receptor co-activator-1 (SRC-1). Based on the activation mechanism of PPARs (the ligand binding to PPAR gamma induces interactions of the receptor with transcriptional co-activators), we performed Western blot and ELISA. These showed that the indomethacin, a PPAR gamma ligand, increased the binding between PPAR gamma and SRC-1 in a ligand dose-dependent manner. These results suggested that the in vitro conformational change of PPAR gamma by ligands was also induced, and increased the levels of the ligand-dependent interaction with SRC-1. Collectively, we developed a novel and useful ELISA system for the mass screening of PPAR gamma ligands. This screening system (based on the interaction between PPAR gamma and SRC-1) may be a promising system in the development of drugs for metabolic disorders.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
1225-8687
pubmed:author
pubmed:issnType
Print
pubmed:day
31
pubmed:volume
36
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
207-13
pubmed:dateRevised
2009-11-19
pubmed:meshHeading
pubmed:year
2003
pubmed:articleTitle
A simple ELISA for screening ligands of peroxisome proliferator-activated receptor-gamma.
pubmed:affiliation
Laboractory of Cellular Biology, Korea Research Institute of Bioscience and Biotechnology, Daejon 305-600, Korea.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Evaluation Studies