Recombinant Human Bile Acid Receptor (NR1H4) Protein (His-SUMO)

Name: Recombinant Human Bile Acid Receptor (NR1H4) Protein (His-SUMO)
Brand: Beta LifeScience
SKU: BLC-08772P
Availability: InStock

Greater than 90% as determined by SDS-PAGE.

Based on the SEQUEST from database of E.coli host and target protein, the LC-MS/MS Analysis result of this product could indicate that this peptide derived from E.coli-expressed Homo sapiens (Human) NR1H4.

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Product Overview

Description	Recombinant Human Bile Acid Receptor (NR1H4) Protein (His-SUMO) is produced by our E.coli expression system. This is a full length protein.
Purity	Greater than 90% as determined by SDS-PAGE.
Uniprotkb	Q96RI1
Target Symbol	NR1H4
Synonyms	BAR; Bile acid receptor; Farnesoid X activated receptor; Farnesoid X receptor; Farnesoid X-activated receptor; Farnesol receptor HRR 1; Farnesol receptor HRR-1; Farnesol receptor HRR1; FXR; HRR 1; HRR1; NR1H4; NR1H4_HUMAN; Nuclear receptor subfamily 1 group H member 4; Retinoid X receptor interacting protein 14; Retinoid X receptor-interacting protein 14; RIP 14; RIP14; RXR interacting protein 14; RXR-interacting protein 14
Species	Homo sapiens (Human)
Expression System	E.coli
Tag	N-6His-SUMO
Target Protein Sequence	MGSKMNLIEHSHLPTTDEFSFSENLFGVLTEQVAGPLGQNLEVEPYSQYSNVQFPQVQPQISSSSYYSNLGFYPQQPEEWYSPGIYELRRMPAETLYQGETEVAEMPVTKKPRMGASAGRIKGDELCVVCGDRASGYHYNALTCEGCKGFFRRSITKNAVYKCKNGGNCVMDMYMRRKCQECRLRKCKEMGMLAECMYTGLLTEIQCKSKRLRKNVKQHADQTVNEDSEGRDLRQVTSTTKSCREKTELTPDQQTLLHFIMDSYNKQRMPQEITNKILKEEFSAEENFLILTEMATNHVQVLVEFTKKLPGFQTLDHEDQIALLKGSAVEAMFLRSAEIFNKKLPSGHSDLLEERIRNSGISDEYITPMFSFYKSIGELKMTQEEYALLTAIVILSPDRQYIKDREAVEKLQEPLLDVLQKLCKIHQPENPQHFACLLGRLTELRTFNHHHAEMLMSWRVNDHKFTPLLCEIWDVQ
Expression Range	1-476aa
Protein Length	Full Length of Isoform 3
Mol. Weight	70.7kDa
Research Area	Transcription
Form	Liquid or Lyophilized powder
Buffer	Liquid form: default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol. Lyophilized powder form: the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose, pH 8.0.
Reconstitution	Briefly centrifuged the vial prior to opening to bring the contents to the bottom. Reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL. It is recommended to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. The default final concentration of glycerol is 50%.
Storage	1. Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. 2. Avoid repeated freeze-thaw cycles. 3. Store working aliquots at 4°C for up to one week. 4. In general, protein in liquid form is stable for up to 6 months at -20°C/-80°C. Protein in lyophilized powder form is stable for up to 12 months at -20°C/-80°C.
Notes	Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Target Details

Target Function	Ligand-activated transcription factor. Receptor for bile acids (BAs) such as chenodeoxycholic acid (CDCA), lithocholic acid, deoxycholic acid (DCA) and allocholic acid (ACA). Plays a essential role in BA homeostasis through the regulation of genes involved in BA synthesis, conjugation and enterohepatic circulation. Also regulates lipid and glucose homeostasis and is involved innate immune response. The FXR-RXR heterodimer binds predominantly to farnesoid X receptor response elements (FXREs) containing two inverted repeats of the consensus sequence 5'-AGGTCA-3' in which the monomers are spaced by 1 nucleotide (IR-1) but also to tandem repeat DR1 sites with lower affinity, and can be activated by either FXR or RXR-specific ligands. It is proposed that monomeric nuclear receptors such as NR5A2/LRH-1 bound to coregulatory nuclear responsive element (NRE) halfsites located in close proximity to FXREs modulate transcriptional activity. In the liver activates transcription of the corepressor NR0B2 thereby indirectly inhibiting CYP7A1 and CYP8B1 (involved in BA synthesis) implicating at least in part histone demethylase KDM1A resulting in epigenomic repression, and SLC10A1/NTCP (involved in hepatic uptake of conjugated BAs). Activates transcription of the repressor MAFG (involved in regulation of BA synthesis). Activates transcription of SLC27A5/BACS and BAAT (involved in BA conjugation), ABCB11/BSEP (involved in bile salt export) by directly recruiting histone methyltransferase CARM1, and ABCC2/MRP2 (involved in secretion of conjugated BAs) and ABCB4 (involved in secretion of phosphatidylcholine in the small intestine). Activates transcription of SLC27A5/BACS and BAAT (involved in BA conjugation), ABCB11/BSEP (involved in bile salt export) by directly recruiting histone methyltransferase CARM1, and ABCC2/MRP2 (involved in secretion of conjugated BAs) and ABCB4 (involved in secretion of phosphatidylcholine in the small intestine). In the intestine activates FGF19 expression and secretion leading to hepatic CYP7A1 repression. The function also involves the coordinated induction of hepatic KLB/beta-klotho expression. Regulates transcription of liver UGT2B4 and SULT2A1 involved in BA detoxification; binding to the UGT2B4 promoter seems to imply a monomeric transactivation independent of RXRA. Modulates lipid homeostasis by activating liver NR0B2/SHP-mediated repression of SREBF1 (involved in de novo lipogenesis), expression of PLTP (involved in HDL formation), SCARB1 (involved in HDL hepatic uptake), APOE, APOC1, APOC4, PPARA (involved in beta-oxidation of fatty acids), VLDLR and SDC1 (involved in the hepatic uptake of LDL and IDL remnants), and inhibiting expression of MTTP (involved in VLDL assembly. Increases expression of APOC2 (promoting lipoprotein lipase activity implicated in triglyceride clearance). Transrepresses APOA1 involving a monomeric competition with NR2A1 for binding to a DR1 element. Also reduces triglyceride clearance by inhibiting expression of ANGPTL3 and APOC3 (both involved in inhibition of lipoprotein lipase). Involved in glucose homeostasis by modulating hepatic gluconeogenesis through activation of NR0B2/SHP-mediated repression of respective genes. Modulates glycogen synthesis (inducing phosphorylation of glycogen synthase kinase-3). Modulates glucose-stimulated insulin secretion and is involved in insulin resistance. Involved in intestinal innate immunity. Plays a role in protecting the distal small intestine against bacterial overgrowth and preservation of the epithelial barrier. Down-regulates inflammatory cytokine expression in several types of immune cells including macrophages and mononuclear cells. Mediates trans-repression of TLR4-induced cytokine expression; the function seems to require its sumoylation and prevents N-CoR nuclear receptor corepressor clearance from target genes such as IL1B and NOS2. Involved in the TLR9-mediated protective mechanism in intestinal inflammation. Plays an anti-inflammatory role in liver inflammation; proposed to inhibit proinflammatory (but not antiapoptotic) NF-kappa-B signaling).; Promotes transcriptional activation of target genes NR0B2/SHP (inducible by unconjugated CDCA), SLC51B/OSTB (inducible by unconjugated CDCA and DCA) and FABP6/IBAP; low activity for ABCB11/BSEP (inducible by unconjugated CDCA, DCA and ACA); not inducible by taurine- and glycine-amidated CDCA.; Promotes transcriptional activation of target genes ABCB11/BSEP (inducible by unconjugated CDCA, DCA and ACA), NR0B2/SHP (inducible by unconjugated CDCA DCA and ACA), SLC51B/OSTB (inducible by unconjugated CDCA and DCA) and FABP6/IBAP; not inducible by taurine- and glycine-amidated CDCA.; Promotes transcriptional activation of target genes NR0B2/SHP (inducible by unconjugated CDCA), SLC51B/OSTB (inducible by unconjugated CDCA and DCA) and IBAP; low activity for ABCB11/BSEP (inducible by unconjugated CDCA, DCA and ACA); not inducible by taurine- and glycine-amidated CDCA.; Promotes transcriptional activation of target genes ABCB11/BSEP (inducible by unconjugated CDCA, ACA and DCA), NR0B2/SHP (inducible by unconjugated CDCA, ACA and DCA), SLC51B/OSTB (inducible by unconjugated CDCA and DCA) and FABP6/IBAP; most efficient isoform compared to isoforms 1 to 3; not inducible by taurine- and glycine-amidated CDCA.
Subcellular Location	Nucleus.; [Isoform 1]: Nucleus.; [Isoform 2]: Nucleus.; [Isoform 3]: Nucleus.; [Isoform 4]: Nucleus.
Protein Families	Nuclear hormone receptor family, NR1 subfamily
Database References	HGNC: 7967 OMIM: 603826 KEGG: hsa:9971 STRING: 9606.ENSP00000447149 UniGene: PMID: 29377207 Activation of FXR inhibits, whereas TGR5 activation may promote, cholangiocarcinoma progression by regulating proliferation, migration and mitochondrial energy metabolism. PMID: 28916388 study demonstrated for the first time a novel target for farnesoid X-activated receptor (FXR) and that the activated receptor alters the acquisition of sperm fertilising ability PMID: 29921626 Low FXR expression is associated with colorectal cancer. PMID: 30106441 Studies indicate that the deregulation of farnesoid X receptor (FXR) may lead to abnormalities of specific organs and metabolic dysfunction [Review]. PMID: 30013008 FXR agonist treatment enhanced TGF-beta-induced epithelial mesenchymal transition(EMT) morphologic changes and FXR antagonist inhibited the effect of TGF-beta;. Thus, FXR activation enhances EMT in hepatocellular carcinoma (HCC) and FXR antagonists may be EMT-suppressing drug candidates. PMID: 29958417 This study provides some data suggesting the possible involvement of FXR in the pathophysiology and development of thyroid neoplasms. In particular, we found that there are differences regarding FXR expression between papillary carcinomas and hyperplastic nodules, being also correlated with some patients' clinicopathological parameters. PMID: 28762281 Data suggest that TGR5 and FXR in intestinal mucosa are important for glucose homeostasis, in particular in metabolic disorders such as type 2 diabetes and obesity. (TGR5 = membrane-type receptor for bile acids TGR5; FXR = farnesoid X receptor) [REVIEW; Congress as Topic] PMID: 27846919 These results suggested that FXR may serve as an important negative regulator for manipulating Smad3 expression, and the FXR/Smad3 pathway may be a novel target for the treatment of renal fibros PMID: 27853248 Loss of FXR or its down-regulation is associated with higher bile acids concentrations and with a pro-tumorigenic phenotype. (Review) PMID: 28400119 Lys-325 is a non-canonical site of SUMOylation of human FXR.CK2 is the priming effector that phosphorylates Ser-327, resulting in enhanced SUMO2 conjugation, which then directs the ubiquitination and degradation of FXR through the recruitment of the SUMO-dependent ubiquitin E3 ligase RNF4. PMID: 28201649 we proposed a model to link FXR to Sp1, which included triggered FXR, p38/MAPK and/or PI3K/AKT signaling and phosphorylated Sp1, to illustrate the potential crosstalk between the two factors. PMID: 28402278 the presented evidence suggested that WA can inhibit HCC cell proliferationand tumorigenesis through miR-22-repressed CCNA2, which was at least partially through FXR regulation PMID: 27738335 The results indicated that epigenetically regulated miR-449a targets CREB5 to increase FXRalpha expression, thereby promoting HBV replication and gene expression. Our findings provide a new understanding of the role of miRNAs in HBV replication PMID: 27138288 In diabetic humans, there is decreased FXR expression in the kidney. FXR plays an important role in Diabetic Kidney Disease. PMID: 27045028 FXR regulates serum triglyceride level in part through PLA2G12B. PMID: 27471003 It regulates the growth of renal adenocarcinoma cells. PMID: 28496032 we conclude that FXR-Gank-TSPs-Stem cells pathway is a key determinant of liver cancer in animal models and in pediatric liver cancer. Our data provide a strong basis for development of FXR-Gank-based therapy for treatment of patients with hepatoblastoma PMID: 28535186 PPARalpha and FXR function coordinately to integrate liver energy balance. PMID: 28287408 These studies investigated in differentiated HepaRG cells and in primary human hepatocytes (PHHs) effects of FXR activation on HBV replication and of infection on the FXR pathway. PMID: 27251172 Treatment with LXR and FXR ligands initiates coated platelet formation, which is thought to support coagulation but results in desensitization to platelet stimuli through inhibition of alphaIIbbeta3 consistent with their ability to inhibit platelet function and stable thrombus formation in vivo. PMID: 28619996 FXR ligands to inhibit platelet activation. PMID: 27758768 Taken together, our data provide the first evidence that FXR suppresses proliferation of human liver cancer cells via the inhibition of the mTOR/S6K signaling pathway. FXR expression can be used as a biomarker of personalized mTOR inhibitor treatment assessment for liver cancer patients. PMID: 27109477 Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy. PMID: 26899873 FXR may promote the proliferation of tumor cells and the hepatocytes in the process of liver regeneration by activating the PDK4-mediated metabolic reprogramming to generate glycolytic intermediates essential for rapid biomass generation, establishing a mechanistic link between cell proliferation and metabolic switch. PMID: 26728993 this is the first report of bile acid derivatives able to antagonize GPBAR1 and and farnesoid X receptor (FXR) modulatory activity. PMID: 26607331 induction of SOCS3 may be a novel mechanism by which FXR exerts its anti-hepatocellular carcinoma effects PMID: 26416445 Mutations in NR1H4 cause progressive familial intrahepatic cholestasis. PMID: 26888176 we drew a conclusion that curcumin attenuated Alcoholic liver disease by modulating lipid deposition in hepatocytes via a Nrf2/FXR activation-dependent mechanism PMID: 26305715 miR-122 is a novel target gene of FXR, and the upregulation of miR-122 by FXR represses the growth of hepatocellular carcinoma cells, suggesting that FXR may serve as a key transcriptional regulator for manipulating miR-122 expression PMID: 26302777 IL-18 repressed FXR mRNA and protein levels in HepG2 cells. PMID: 26292095 FXR signalling in ileum biopsies of humans positively correlates with body mass index. PMID: 26670557 FXR activation in L cells decreases proglucagon expression by interfering with the glucose-responsive factor Carbohydrate-Responsive Element Binding Protein (ChREBP) and GLP-1 secretion by inhibiting glycolysis. PMID: 26134028 FXR is decreased in obese animal models associated with INS resistance. Regulation of bile acids and FXR in the stage of obesity may prevent more metabolism disorders. PMID: 26488943 These results provide important information to prioritize chemicals for further investigation, and suggest possible modes of action of compounds in FXR signaling. PMID: 25257666 FXR may regulate SOD3 expression to suppress reactive oxygen species production, resulting in decreasing JNK activity. PMID: 25496033 Liver nuclear receptors, FXR and SHP, and bile acid transporters, NTCP and BSEP, are associated with the progression of NAFLD. PMID: 26019035 Three FXR gene variants (rs35724, rs11110385, rs11110386) were identified as potential susceptibility factors for cholelithiasis in a German cohort in gender- and weight-dependent manners PMID: 25242139 these data demonstrate that copper-mediated nuclear receptor dysfunction disrupts liver function in WD and potentially in other disorders associated with increased hepatic copper levels. PMID: 26241054 FXR agonist, GW4064, upregulates adipokine expression in preadipocytes and HepG2 cells. PMID: 25400456 NHR1H4 genotype increases the risk for spontaneous bacterial peritonitis in live cirrhosis patients. PMID: 25086996 Results show that HRG is a novel transcriptional target gene of FXR in human hepatoma cells, human upcyteVR primary hepatocytes and 3D human liver microtissues in vitro and in mouse liver in vivo. PMID: 25363753 established genome-wide human FXR binding and transcriptome profiles. These results will aid in determining the human FXR functions, as well as judging to what level the mouse models could be used to study human FXR functions PMID: 25198545 our data showed that bile acid-activated FXR stimulates miR-22-silenced CCNA2, a novel pathway for FXR to exert its protective effect in the gastrointestinal tract. PMID: 25596928 AB23A produces protective effect against ANIT-induced hepatotoxity and cholestasis, due to FXR-mediated regulation of transporters and enzymes. PMID: 25655198 Compared with normal gallbladder tissues, FXR expression was decreased and MCL1 expression was increased in GBC, during progression of tumor node metastasis (TNM) stage PMID: 25043081 Intestinal nuclear bile acid farnesoid X receptor is regulated transcriptionally by CDX2. PMID: 25138215 significant differences at the distal (-1890) and proximal promoter (-358) CpG sites of the FXR/NR1H4 and at the distal PXR/NR1I2 (-1224) promoter, which were consistently less methylated in ICP cases when compared with controls. PMID: 24498169 show that FXR interacts with and is O-GlcNAcylated by O-GlcNAc transferase in its N-terminal AF1 domain PMID: 24037988 NR1H4 methylation is associated with colon cancer. PMID: 24169962

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Proteins are sensitive to heat, and freeze-drying can preserve the activity of the majority of proteins. It improves protein stability, extends storage time, and reduces shipping costs. However, freeze-drying can also lead to the loss of the active portion of the protein and cause aggregation and denaturation issues. Nonetheless, these adverse effects can be minimized by incorporating protective agents such as stabilizers, additives, and excipients, and by carefully controlling various lyophilization conditions.

Commonly used protectant include saccharides, polyols, polymers, surfactants, some proteins and amino acids etc. We usually add 8% (mass ratio by volume) of trehalose and mannitol as lyoprotectant. Trehalose can significantly prevent the alter of the protein secondary structure, the extension and aggregation of proteins during freeze-drying process; mannitol is also a universal applied protectant and fillers, which can reduce the aggregation of certain proteins after lyophilization.

Our protein products do not contain carrier protein or other additives (such as bovine serum albumin (BSA), human serum albumin (HSA) and sucrose, etc., and when lyophilized with the solution with the lowest salt content, they often cannot form A white grid structure, but a small amount of protein is deposited in the tube during the freeze-drying process, forming a thin or invisible transparent protein layer.

Reminder: Before opening the tube cap, we recommend that you quickly centrifuge for 20-30 seconds in a small centrifuge, so that the protein attached to the tube cap or the tube wall can be aggregated at the bottom of the tube. Our quality control procedures ensure that each tube contains the correct amount of protein, and although sometimes you can't see the protein powder, the amount of protein in the tube is still very precise.

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