Fxr transactivation assay
WebAug 1, 2011 · FXR has important roles in controlling lipid and glucose levels. FXR activity is regulated by transcriptional cofactors, which catalyze PTMs of FXR as well as histones. … WebNov 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 ...
Fxr transactivation assay
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WebSep 19, 2007 · The farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily that is highly expressed in liver, kidney, adrenals, and intestine. ... 2.4 Quantitative real-time RT–PCR assay of eNOS. ... tk-luciferase reporter gene that contains three copies of the eNOS/IR2 element was generated and tested for FXR … WebTo identify compounds that modulate FXR transactivation at the cellular level, we first screen compounds from the Tox21 10 K compound library in an FXR-driven beta …
WebJan 1, 2024 · The assay that is used to determine to transcriptional activity of full length FXR on its response element BSEP promoter is based on a reporter construct containing FXR expression plasmid and BSEP luciferase gene reporter. The null-renilla luciferase were co-transfected as internal control for normalization. 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 ...
WebJan 1, 2024 · Based on our ongoing pursuit on isoxazole-type nonsteroidal FXR modulators, we reported herein the structural simplification and optimization on a clinical FXR agonist … WebEnter the email address you signed up with and we'll email you a reset link.
WebWhen 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.
WebCat. No. Product Name CAS No. Information; PC-62478: BILH-434. 760169-28-6: BILH-434 is a potent HPV11 E1/E2/DNA complex inhibitor that binds to the transactivation domain (TAD) of E2 protein with a Kd of 40 nM, has an IC50 of 180 nM in the E1-E2-ori complex formation assay.. banda bWebJan 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 … banda b105WebInduction of FXR-target gene expression by FXR ligands is abolished in mice when guggulsterones are coadministered (Urizar et al., 2002; Wu et al., 2002). Other research shows that guggulsterones enhance the action of specific FXR ago-nists toward bile salt excretory protein gene expression in vivo and may function as a selective FXR modulator … arti dari sifat rasul tabligh yaituWebrecruitment, 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 … arti dari sifat gereja yang katolik adalahWebFeb 18, 2016 · Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis - PMC Back to Top Skip to main content An official website of the United States government Here's how you know The .gov means it’s official. Federal government websites often end in .gov or .mil. arti dari sifat iradah adalahWebCompound 10a showed significantly improved activity for FXR, compared with our previously identified hit compound XJ034.. Compound 10a showed high selectivity to FXR and had no cytotoxicity to HepG2 cells.. Compound 10a (100 mg/kg) improved hyperlipidemia, hepatic steatosis and insulin resistance in DIO mice.. Compound 10a … banda b106WebJan 1, 2024 · FXR represses the transcriptional activity of hepatic Cyp7a1 and Cyp8b1 by upregulating the expression of SHP. FXR stimulates the synthesis of the FGF-15/19-FGFR4 pathways to inhibit CYP7A1 and CYP8B1 expression. FXR regulates key genes involved in BA transport, reabsorption, conjugation and detoxification, such as NTCP, BSEP, MDR3 … arti dari signifikan