Fxr transactivation assay
WebMar 17, 2024 · The farnesoid X receptor (FXR) is a major nuclear receptor of bile acids; its activation suppresses sterol regulatory element-binding protein 1c (SREBP1c)-mediated lipogenesis and decreases the lipid contents in the liver. WebJun 15, 2012 · In vitro full length FXR transactivation assay in HeLa cells transfected with FXR/RXR, BSEP-pGL3 and pRL-SV40. Compounds were ordered as they appear on the SOM neurons (numbers beneath the bars) and tested at 10 μM. Due to toxicity pentamidine and sorafenib were tested at 3 μM, atorvastatin at 1 μM and ouabain at 0.03 μM.
Fxr transactivation assay
Did you know?
WebJan 5, 2024 · We further confirmed its FXR agonistic activity by coactivator recruitment assay, FXR responsive element (FXRE)-specific transactivation assay, and SREBP transactivation assay. We explored its selectivity to FXR by evaluating the activity for PPARα/γ/δ and Takeda G protein-coupled receptor 5 (TGR5), as well as its cytotoxicity … WebJan 13, 2024 · Since transcriptional activities of NRs may also be modulated by post translational modifications (PTMs) 40,41, the PTMs of FXR were explored. Results from Co-IP assay showed that FXR SUMOylation ...
WebThe farnesoid X receptor (FXR) is a member of the nuclear family of receptors and has emerged as a key player in the control of numerous metabolic pathways. Bile acids and … Webrecruitment, GST pull-down assay, FXR transactivation, and quantitative real-time PCR for examining the expression of FXR targets. Our results indicate that CDCA is a full FXR …
WebMay 1, 2024 · ( A) At 10 µM, 16 significantly enhances transactivation efficacy of FXR agonists 1 – 3 in a full-length FXR reporter gene assay. … WebJan 13, 2024 · These results reveal a novel function of the basal autophagy-NRF2 axis for the regulation of FXR transactivation, and shed light on a potential therapeutic strategy in metabolic disease. ... 1 (KEAP1), an adaptor component for Cullin3-based E3 ubiquitin ligase complex. Farnesoid x receptor (FXR/NR1H4) is a ligand-dependent transcription …
WebJan 29, 2015 · Moreover, we experimentally validated that FXR antagonism of NSAIDs is a potential molecular mechanism of DILI, using yeast two-hybrid assay, mammalian transactivation assays, qRT-PCR and western ...
WebSep 26, 2014 · The farnesoid X receptor (FXR) regulates the homeostasis of bile acids, lipids, and glucose. Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. We used a cell-based human FXR β-lactamase (Bla) reporter gen … gips hospital and de-addiction centreWebJan 7, 2016 · Even if less potent in transactivation assay than 6-ethylchenodeoxycholic acid, 6-ECDCA/OCA (6), the most potent steroidal FXR agonist generated so far, the potency of compound 5 in inducing the ... fulton county humane society gaWebMar 2, 2004 · In this study, we systematically characterized the FXR agonist activities of these bile acids using a series of cell-free and cell-based assays including coactivator … gips intrinsic plusWebWhen presence of FXR and RXRα, the FXRE is activated, subsequently, the luciferase gene is transcribed. Such a transactivation assay cam be used to verify the antagonistic effect of H7 on FXR. Finally, transactivation assay was further carried out to verify the antagonistic effect of H7 on FXR. gips intertoysWebAssay Type Time Activity Description Data Sources; HCA2: 2.5 μM: Function Assay-Inhibits p38 mediated MK2 activation: 17964780: Hela-Function Assay-Inhibits Tat-induced HIV1 LTR transactivation in human HeLa cells with IC50 of 0.1 μM: 18926711: hESCs: 5 μM: Growth Inhibition Assay-Induces cardiomyogenic activity assessed as cell growth: … gips in englishWebNov 21, 2013 · To measure FXR agonistic activity, we performed a cellular transactivation assay using an FXR BSEP-luciferase reporter gene assay in HEK293T cells as previously described [36]. The assay that is ... gips icd 9WebFeb 25, 2024 · The potency of INT-767 (EC 50 = 7 ± 1.5 nM) for FXR was approximately 10-fold higher than that of INT-747 (76 ± 4.3 nM) in the AlphaScreen coactivator recruitment assay. Moreover, FXR can be... We would like to show you a description here but the site won’t allow us. gip silpc isle