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Human FXR (LBD)-GAL4 (DBD) Stable Cell Line-HEK 293T(UAS-bla)

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Cat.No.
CSC-RN0003
Background
The farnesoid X receptor (FXR) is a nuclear hormone receptor and can function as a ligand inducible transcription factor capable of acting as a co-repressor and/or co-activator for gene expression. Nuclear receptors contain a series of conserved domains or regions. These domains/regions include a variable NH2-domain (A/B region), a conserved DNA-binding domain (DBD or region C), a linker region (region D), a ligand binding domain (LBD or region E), and in some receptors a variable COOHterminal (region F).
The FXR nuclear receptor forms a heterodimer with RXR (retinoid X receptor) that recognizes an inverted repeat of the AGGTCA sequence with no spacing and 1 base-spacing. The FXR-RXR heterodimer can recognize additional direct repeats with different binding affinities. When bound the FXR-RXR heterodimer can function as a transcription activator or inhibitor. When a ligand interacts with the FXR ligand binding domain the receptor undergoes conformational changes. These conformational changes lead to a decrease in the affinity of transcription co-repressors and the interaction with transcription co-activators. These co-activators and co-repressors regulate gene transcription by interacting with the transcriptional pre-initiation complex and histone acetyl transferases. The interaction of nuclear receptors and FXR with these co-activators and corepressors may be ligand specific. FXR is activated by bile acids and regulates the expression of genes involved in bile acid synthesis, cholesterol metabolism, and plasma triglyceride concentrations. The primary agonist for FXR is chenodeoxycholic acid (CDCA). Additional bile acids function as partial agonists for FXR including: deoxycholic acid (DCA), cholic acid (CA), and ursodeoxycholic acid (UDCA). FXR is expressed in the liver, intestine, kidney and adrenal cortex. FXR reduces bile acid concentration in heptocytes by repressing genes involved in the bile acid biosynthetic pathway (CYP7A1, CYP8B1, and CYP27A1), and regulates triglyceride and lipoprotein metabolism by increasing the expression of apolipoprotein and lipoprotein enzymes (PLTP and APOCII).
Growth Properties
Adherent
Morphology
Epithelial
Host Cell
HEK 293T
Ship
Dry ice
Gene Information
Official Symbol
NR1H4
Synonyms
NR1H4; nuclear receptor subfamily 1, group H, member 4; bile acid receptor; FXR; HRR 1; HRR1; RIP14; farnesol receptor HRR-1; RXR-interacting protein 14; farnesoid X nuclear receptor; farnesoid X-activated receptor; retinoid X receptor-interacting protein 14; BAR; HRR-1; MGC163445;
Gene ID
MIM
UniProt ID
Q96RI1
Chromosome Location
12q23.1
Pathway
Bile secretion, organism-specific biosystem; Bile secretion, conserved biosystem; Gene Expression, organism-specific biosystem; Generic Transcription Pathway, organism-specific biosystem; Nuclear Receptor transcription pathway, organism-specific biosystem; Nuclear receptors in lipid metabolism and toxicity, organism-specific biosystem; RXR and RAR heterodimerization with other nuclear receptor, organism-specific biosystem;
Function
RNA polymerase II distal enhancer sequence-specific DNA binding; RNA polymerase II transcription factor binding transcription factor activity involved in positive regulation of transcription; bile acid binding; bile acid binding; ligand-activated sequence-specific DNA binding RNA polymerase II transcription factor activity; ligand-dependent nuclear receptor binding; metal ion binding; protein binding; receptor activity; sequence-specific DNA binding; sequence-specific DNA binding transcription factor activity; sequence-specific distal enhancer binding RNA polymerase II transcription factor activity; steroid hormone receptor activity; thyroid hormone receptor activity; transcription coactivator activity; transcription corepressor activity; zinc ion binding;

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