PMID- 16171942 OWN - NLM STAT- MEDLINE DCOM- 20060124 LR - 20161124 IS - 0303-7207 (Print) IS - 0303-7207 (Linking) VI - 242 IP - 1-2 DP - 2005 Oct 20 TI - 5-(3,5-Di-tert-butyl-4-hydroxybenzylidene) thiazolidine-2,4-dione modulates peroxisome proliferators-activated receptor gamma in 3T3-L1 adipocytes: roles as a PPARgamma ligand. PG - 96-102 AB - Based on the binding between peroxisome proliferators-activated receptor gamma (PPARgamma) and steroid receptor co-activator-1 (SRC-1), an enzyme-linked immunosorbent assay (ELISA) was used to screen new PPARgamma ligands from various benzylidinethiazole derivatives, which have anti-inflammatory activity. Among those derivatives, 5-(3,5-di-tert-butyl-4-hydroxybenzylidene) thiazolidine-2,4-dione (BTZD) increased the binding between PPARgamma and SRC-1. BTZD was found to induce adipogenesis and PPARgamma trans-activation in 3T3-L1 pre-adipocyte, and increased the binding between PPARgamma and SRC-1 in in vitro binding assay and complex consisting of PPARgamma and SRC-1 in the co-immunoprecipitaion. Chromatin immunoprecipitation (ChIP) analysis revealed that BTZD induced the binding of PPARgamma-SRC-1 complex to PPAR response element (PPRE) in the same pattern of other PPARgamma ligand. From these studies, we have identified and studied the function of a new PPARgamma ligand, BTZD. We suggest that BTZD can be used as a modulator of PPARgamma. This study applying ELISA and ChIP assay can offer new methods to screen PPARgamma ligand and understand the effects of PPARgamma ligands on inflammation. FAU - Cho, Min-Chul AU - Cho MC AD - Laboratory of Cell Biology, Korea Research Institute of Bioscience and Biotechnology, P.O. Box 115, Daejeon 305-600, Republic of Korea. FAU - Lee, Woo Song AU - Lee WS FAU - Hong, Jin-Tae AU - Hong JT FAU - Park, Se-Won AU - Park SW FAU - Moon, Dong-Cheul AU - Moon DC FAU - Paik, Sang-Gi AU - Paik SG FAU - Yoon, Do-Young AU - Yoon DY LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Ireland TA - Mol Cell Endocrinol JT - Molecular and cellular endocrinology JID - 7500844 RN - 0 (5-(3,5-di-tert-butyl-4-hydroxybenzylidene)thiazolidine-2,4-dione) RN - 0 (Ligands) RN - 0 (PPAR gamma) RN - 0 (Recombinant Fusion Proteins) RN - 0 (Thiazolidinediones) RN - 0 (Transcription Factors) RN - EC 2.3.1.48 (Histone Acetyltransferases) RN - EC 2.3.1.48 (Ncoa1 protein, mouse) RN - EC 2.3.1.48 (Nuclear Receptor Coactivator 1) SB - IM MH - 3T3-L1 Cells MH - Adipocytes/*drug effects/metabolism MH - Animals MH - Binding Sites MH - Fibroblasts/cytology/drug effects MH - Genes, Reporter MH - Histone Acetyltransferases MH - Ligands MH - Lipid Metabolism/drug effects MH - Mice MH - Nuclear Receptor Coactivator 1 MH - PPAR gamma/*metabolism MH - Promoter Regions, Genetic/genetics MH - Protein Binding/drug effects MH - Recombinant Fusion Proteins MH - Thiazolidinediones/*metabolism/*pharmacology MH - Transcription Factors/metabolism MH - Transcriptional Activation/drug effects/genetics EDAT- 2005/09/21 09:00 MHDA- 2006/01/25 09:00 CRDT- 2005/09/21 09:00 PHST- 2005/07/19 00:00 [received] PHST- 2005/08/04 00:00 [accepted] PHST- 2005/09/21 09:00 [pubmed] PHST- 2006/01/25 09:00 [medline] PHST- 2005/09/21 09:00 [entrez] AID - S0303-7207(05)00277-7 [pii] AID - 10.1016/j.mce.2005.08.005 [doi] PST - ppublish SO - Mol Cell Endocrinol. 2005 Oct 20;242(1-2):96-102. doi: 10.1016/j.mce.2005.08.005.