Mouse Monoclonal Anti-SHP/NR0B2/Nuclear Receptor SHP Antibody (1A11) [PerCP]. Validated: WB, ELISA, ICC/IF. Tested Reactivity: Human. 100% Guaranteed.
The liver receptor homolog-1 (LRH-1) also known as NR5A2 (nuclear receptor subfamily 5, group A, member 2) is a protein that in humans is encoded by the NR5A2 gene.[1][2] LRH-1 is a member of the nuclear receptor family of intracellular transcription factors. LRH-1 plays a critical role in the regulation of development, cholesterol transport, bile acid homeostasis and steroidogenesis.[3][4][5] LRH-1 is important for maintaining pluripotence of stem cells during embryonic development.[6] ...
TY - JOUR. T1 - Expression of glucocorticoid and progesterone nuclear receptor genes in archival breast cancer tissue. AU - Smith, Robert A.. AU - Lea, Rod A.. AU - Curran, Joanne E.. AU - Weinstein, Stephen R.. AU - Griffiths, Lyn R.. PY - 2002/12/4. Y1 - 2002/12/4. N2 - Background: Previous studies in our laboratory have shown associations of specific nuclear receptor gene variants with sporadic breast cancer. In order to investigate these findings further, we conducted the present study to determine whether expression levels of the progesterone and glucocorticoid nuclear receptor genes vary in different breast cancer grades. Methods: RNA was extracted from paraffin-embedded archival breast tumour tissue and converted into cDNA. Sample cDNA underwent PCR using labelled primers to enable quantitation of mRNA expression. Expression data were normalized against the 18S ribosomal gene multiplex and analyzed using analysis of variance. Results: Analysis of variance indicated a variable level of ...
The constitutive androstane receptor (CAR, NR1I3) is a central regulator of xenobiotic metabolism. CAR activation induces hepatic expression of detoxification enzymes and transporters and increases liver size. Here we show that CAR-mediated hepatomegaly is a transient, adaptive response to acute xen …
There are no specific protocols for Recombinant Human Constitutive androstane receptor protein (ab81846). Please download our general protocols booklet
Rabbit Anti-NR0B2 Polyclonal Antibody,Nuclear receptor subfamily 0 group B member 2; Orphan nuclear receptor SHP; Small heterodimer partner,The protein encoded by NR0B2 (Nuclear Receptor Subfamily 0 Group B Member 2) is an unusual orphan receptor that contains a putative ligand-binding domain but lacks a conventional DNA-binding domain. NR0B2 product is a member of the nuclear hormone receptor family, a group of transcription factors regulated by small hydrophobic hormones, a subset of which do not have known ligands and are referred to as orphan nuclear receptors. The protein has been shown to interact with retinoid and thyroid hormone receptors, inhibiting their ligand-dependent transcriptional activation.
Examples of orphan receptors are found in the G protein-coupled receptor (GPCR)[2][3][4] and nuclear receptor[5][6][7] families. If an endogenous ligand is found, the orphan receptor is "adopted" or "de-orphanized"[8]. An example is the nuclear receptor Farnesoid X receptor (FXR) and the GPCR TGR5/GPCR19/G protein-coupled bile acid receptor, both of which are activated by bile acids.[9] Adopted orphan receptors in the nuclear receptor group include FXR, liver X receptor (LXR), and peroxisome proliferator-activated receptor (PPAR). Another example of an orphan receptor site is the PCP binding site in the NMDA receptor,[10] a type of ligand-gated ion channel. This site is where the recreational drug PCP works, but no endogenous ligand is known to bind to this site. GPCR orphan receptors are usually given the name "GPR" followed by a number, for example GPR1. In the GPCR family, nearly 100 receptor-like genes remain orphans.[11] ...
Maxacalcitol 22-Oxacalcitriol is a Vitamin D3 analog which is Non-calcemic as well as a VDR ligand. 22-Oxacalcitriol has been shown to decrease parathyroid hormone (PTH) mRNA expression in vitro. Additionally has been noted to exhibit similar effects to calcitriol in. ...
Patrick Griffin, chair of the Scripps Research Department of Molecular Therapeutics and director of the Translational Research Institute at Scripps Florida, has won a three-year grant of more than $1.2 million from the National Cancer Institute of the NIH to develop a series of high-throughput screening tests that will help speed the discovery of potential small molecule therapies for breast cancer and cardiovascular disease. The tests will focus on identifying ligands for the orphan nuclear receptor liver receptor homolog-1 or LRH-1, which plays a crucial role in hormone-driven breast cancer through its regulation of genes involved in hormone biosynthesis as well as fat and cholesterol metabolism-key risk factors in cardiovascular disease ...
Title:Medicinal Chemistry and Pharmacological Effects of Farnesoid X Receptor (FXR) Antagonists. VOLUME: 14 ISSUE: 19. Author(s):Christina Lamers, Manfred Schubert-Zsilavecz and Daniel Merk. Affiliation:Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max-von-Laue-Str. 9, 60438 Frankfurt (Main), Germany.. Keywords:Atherosclerosis, cancer, FXR antagonists, FXR knockout, glucose homeostasis, guggulsterone, lipid homeostasis, liver disorders, metabolic disorders, selective bile acid receptor modulators (SBARMs).. Abstract:The nuclear bile acid sensor farnesoid X receptor (FXR) constitutes a rising target for the treatment of a variety of diseases including metabolic disorders, inflammation and certain forms of cancer. While the research on FXR agonists has yielded many compounds and first clinical candidates, only few FXR antagonists have been discovered so far and the knowledge about their in vivo effects is quite narrow. We have evaluated available in vitro and in vivo studies ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
The growth arrest and DNA damage-inducible 45 (Gadd45) proteins act in many cellular processes. In the liver, Gadd45b (encoding Gadd45β) is the gene most strongly induced early during both compensatory regeneration and drug-induced hyperplasia. The latter response is associated with the dramatic and rapid hepatocyte growth that follows administration of the xenobiotic TCPOBOP (1,4-bis[2-(3,5)-dichoropyridyloxy] benzene), a ligand of the nuclear receptor constitutive androstane receptor (CAR). Here, we have shown that Gadd45b-/- mice have intact proliferative responses following administration of a single dose of TCPOBOP, but marked growth delays. Moreover, early transcriptional stimulation of CAR target genes was weaker in Gadd45b-/- mice than in wild-type animals, and more genes were downregulated. Gadd45β was then found to have a direct role in transcription by physically binding to CAR, and TCPOBOP treatment caused both proteins to localize to a regulatory element for the CAR target gene ...
Background: Small heterodimer partner (SHP; NR0B2) is an atypical orphan nuclear receptor lacking DNA binding domain. SHP directly modulates the activities of other nuclear receptors and regulates a variety of cellular events such as cell differentiation, proliferation, and metabolism in various tissues. However, the role of SHP in heart has not yet been elucidated. Thus, in this study, we tried to investigate the functional roles of SHP in heart physiology and in the development of cardiac hypertrophy.. Methods and Results: We observed that SHP knock-out mice elicited cardiac hypertrophic features determined by heart weight to body weight or to tibia length ratios. Fetal genes, such as atrial natriuretic factor (ANF) or beta myosin heavy chain (βMHC) were significantly up-regulated in SHP knockout mice heart. In neonatal rat ventricular cardiomyocytes (NRVCs), phenylephrine (PE) reduced promoter activation of SHP and decreased protein level of SHP. Adenovirus-mediated over-expression of SHP ...
The constitutive androstane receptor (CAR) also known as nuclear receptor subfamily 1, group I, member 3 is a protein that in humans is encoded by the NR1I3 gene. CAR is a member of the nuclear receptor superfamily and along with pregnane X receptor (PXR) functions as a sensor of endobiotic and xenobiotic substances. In response, expression of proteins responsible for the metabolism and excretion of these substances is upregulated. Hence, CAR and PXR play a major role in the detoxification of foreign substances such as drugs. Androstenol and several isomers of androstanol, androstanes, are endogenous antagonists of the CAR, and despite acting as antagonists, were the basis for the naming of this receptor. More recently, dehydroepiandrosterone (DHEA), also an androstane, has been found to be an endogenous agonist of the CAR. CAR is a member of the nuclear receptor superfamily, and is a key regulator of xenobiotic and endobiotic metabolism. Unlike most nuclear receptors, this transcriptional ...
Maternal obesity is associated with dysregulation of glucose and lipid metabolism with consequent exposure of the fetus to an abnormal metabolic milieu. It is recognized that maternal obesity predisposes offspring to chronic kidney disease (CKD). We aimed to determine whether the nuclear Farnesoid X receptor (FXR), known to play a role in maintaining homeostasis of glucose and lipid metabolism, is involved in renal injury in offspring of obese mothers. Maternal obesity was established in a rat model by feeding dams with high-fat diet prior to and during pregnancy and lactation. The offsprings kidneys were examined at postnatal Day 1and Day 20. Human kidney 2 (HK2) cells were exposed to high glucose with or without the FXR agonist GW4064 or when FXR mRNA was silenced. Glucose intolerance in the offspring of obese mothers was evident at weaning, with associated downregulation of renal FXR expression and upregulation of monocyte chemoattractant protein-1 (MCP-1) and transforming growth factor-β1 (TGF-β1
TY - JOUR. T1 - Recent advances in the development of farnesoid X receptor agonists. AU - Ali, Ahmad H.. AU - Carey, Elizabeth J.. AU - Lindor, Keith. PY - 2015/1/1. Y1 - 2015/1/1. N2 - Farnesoid X receptors (FXRs) are nuclear hormone receptors expressed in high amounts in body tissues that participate in bilirubin metabolism including the liver, intestines, and kidneys. Bile acids (BAs) are the natural ligands of the FXRs. FXRs regulate the expression of the gene encoding for cholesterol 7 alpha-hydroxylase, which is the rate-limiting enzyme in BA synthesis. In addition, FXRs play a critical role in carbohydrate and lipid metabolism and regulation of insulin sensitivity. FXRs also modulate live growth and regeneration during liver injury. Preclinical studies have shown that FXR activation protects against cholestasis-induced liver injury. Moreover, FXR activation protects against fatty liver injury in animal models of nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis ...
Liver receptor homolog-1 (LRH-1; NR5A2) is a member of the NR5A subfamily of nuclear receptors (NRs) for which there are two members (Fayard et al., 2004). LRH-1 and steroidogenic factor-1 (SF-1; NR5A1) both bind to identical DNA consensus sequences (response elements) in promoter regions of their target genes and both bind DNA as monomers (Krylova et al., 2005; Li et al., 2005; Solomon et al., 2005). LRH-1 and SF-1 are differentially expressed in tissues and thus are likely to have nonoverlapping, nonredundant functions. Whereas SF-1 is confined to steroidogenic tissues where it plays a critical role in the regulation of development, differentiation, steroidogenesis, and sexual determination (Broadus et al., 1999; Lavorgna et al., 1991; Luo et al., 1994), LRH-1 is highly expressed in tissues of endodermal origin and is essential for normal intestinal and pancreatic function. In the liver, LRH-1 regulates cholesterol metabolism and bile acid homeostasis (Francis et al., 2003). Most NRs require ...
TLX was recently shown to be expressed in type B cells in the LV (Liu et al., 2010). In agreement with this finding, our inducible lineage tracing further demonstrated that Tlx-expressing cells give rise to both type-1 cells in the SGZ and type B cells in the SVZ. This implies a much broader role of TLX in the regulation of neurogenic stem cells in the adult brain. Consequently, deletion of Tlx leads to completely abolished neurogenesis in both of the neurogenic regions (Shi et al., 2004; Liu et al., 2008; Zhang et al., 2008). Type-1/B cells are slowly dividing stem cells that give rise to transiently but rapidly amplifying type-2/C cells (Kriegstein and Alvarez-Buylla, 2009). Interestingly, both active and inactive NSCs are derived from Tlx-expressing cells. We cannot unambiguously differentiate which of the two types of NSCs express Tlx due to the lack of a sensitive antibody that recognizes endogenous TLX in the adult neurogenic regions. Nevertheless, three pieces of data indicate that Tlx is ...
Plasmids. The full-length mammalian expression vectors encoding human PXR (Lehmann et al., 1998) and mouse PXR (Kliewer et al., 1998) were described previously. The pGEX-PXR ligand-binding domain (LBD) fusion protein also was described previously (Kliewer et al., 1998). The mammalian expression vector encoding human HNF4α was described previously (Wisely et al., 2002). The steroid receptor activator 1 (SRC-1) expression vector was described previously (Onate et al., 1995). The XREM-SPAP reporter gene was constructed using PCR primers to amplify XREM and insert it into the pTAL-SEAP (BD Biosciences Clontech, Palo Alto, CA) using KpnI and BglII restriction sites.. Nuclear Receptor Panel Screen. CV-1 cells were maintained and transiently transfected as described previously (Moore and Kliewer, 2000). The following receptors were transfected as Gal4-LBD chimera constructs (PPARα, PPARδ, PPARγ, retinoic acid receptor α, vitamin D receptor, TRα, and TRβ) with a UAS(5X)-tk-Luciferase reporter as ...
Human nuclear receptors control the expression of genes in response to the binding of small signalling molecules in the body. Many compounds that are in the environment are classed as endocrine-disrupting chemicals as they are thought to directly bind nuclear receptors and change gene expression patterns, leading to harmful physical effects. While many of these compounds are harmless individually, the body is constantly exposed to mixtures of these compounds in the environment. It has long been known that combinations of these chemicals can have additive, antagonistic or synergistic effects, but there has been no understanding of the molecular basis for these effects.. The teams of Patrick Balaguer and William Bourguet of INSERM, CNRS and the University of Montpellier used extensive screening methods and biophysical characterisation to identify two endocrine-disrupting chemicals that act synergistically on a human nuclear receptor, the pregnane X receptor (PXR). The two compounds identified are ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Nuclear receptors are a class of intracellular proteins that sense and respond to a variety of endogenous hormones, vitamins, and xenobiotic endocrine disruptors by modulating gene expression. These proteins have well-established roles in the regulation of energy balance and the skeletal system, and they are emerging as important players in other areas of human physiology and disease. Humans have 48 nuclear receptors that all possess an N-terminal transactivation domain, a highly conserved central region DNA-binding domain, and a C-terminal ligand-binding domain. Ligand binding results in the transactivation of specific genes within a given tissue. Notably, a number of nuclear receptors do not have a known endogenous ligand and structural studies indicate that they may not bind ligands at all, but instead recruit other nuclear receptors or chromatin modifiers to control gene expression. Nuclear receptor activity can be modulated through interactions with other nuclear receptors or ...
Principal Investigator:SHUDO Koichi, Project Period (FY):1993 - 1995, Research Category:Grant-in-Aid for Developmental Scientific Research (B), Research Field:医薬分子機能学
The first tissue to show a clear NR enrichment during development was the maternally provided yolk, which serves as a repository of the biological fuels and building blocks required for embryonic development and hatching. In many cases, these molecules are broken down or released as required from more complex storage or precursor molecules. Ecdysone, for example, which is provided maternally, is not required until mid-embryogenesis. Until that time, it is stored in the yolk linked via phosphate bonds to carrier proteins (Hoffmann and Lagueux 1985; Lagueux et al. 1977, 1981; Bownes et al. 1988a,b). Its release at mid-embryogenesis leads to EcR activity in the midgut and surrounding amnioserosa, with subsequent downstream NR expression and activities in both tissues (Palanker et al. 2006).. Appropriately, the yolk ends up being engulfed by the midgut, which is another common site of NR expression. This ongoing expression in the midgut, and other parts of the gut, is consistent with the roles of ...
We have demonstrated in the present study that the regulatory subunit RIIβ of PKA can interact with a CRE both physically and functionally. Our results showing that the RIIβ is a CRE transcription factor raises the possibility for an entirely different mechanism for cAMP regulation of gene expression. An established mechanism of cAMP/CRE-regulated transcription involves the CREB/ATF family of transcription factors. However, the CREB/ATF transcription factor family is unlikely to mediate all transcriptional responses to cAMP during development, differentiation, and endocrine homeostasis. The recent demonstration of CREB/ATF-independent cAMP gene regulation through orphan nuclear hormone receptor confirms the presence of multiple mechanisms for cAMP-regulated transcription (24, 25).. The function of R subunit in PKA has been confined to its inhibition of the C subunit. Recently, however, binding of R subunit to proteins other than the C subunit of PKA has been explored with the yeast two-hybrid ...
McNulty, BC, Young, GB, Pielak, GJ. 2006. Macromolecular crowding in the Escherichia coli periplasm maintains α-synuclein disorder. Journal of Molecular Biology, 355: 893-897.. McNulty, B. C., Tripathy, A., Young, G. B., Orans, J., Charlton, L. M. and Pielak, G. J. (2006) Temperature- Induced Reversible Conformational Change in the First 100 Residues of Alpha-Synuclein. Protein Science 15:602-608.. Lentz, BR. 2006. Seeing is Believing: the Stalk Intermediate. Biophysical Journal, 91, 2747-8, 2006 (mini-review to highlight a recent BJ paper).. 2005. Kevin A. Wilkinson, Edward J. Merino, and Kevin M. Weeks. 2005. RNA SHAPE Chemistry Reveals Nonhierarchical Interactions Dominate Equilibrium Structural Transitions in tRNA Asp Transcripts. J. Am. Chem. Soc. 127:4659-4667.. Ortlund, EA, Lee, Y, Solomon, IH, Hager, JM, Safi, R, Choi, Y, Guan, Z, Tripathy, A, Raetz, CR, McDonnell, DP, Moore, DD, Redinbo, MR. 2005. Modulation of human nuclear receptor LRH-1 activity by phospholipids and SHP. Nat Struct ...
Our laboratory is interested in understanding how autoreactive B cells, despite chronic antigen engagement of the B cell receptor, are restrained from inappropriate activation and differentiation. We are interested in how this process is disrupted in autoimmune disease, and how tolerance mechanisms can be harnessed to treat autoimmunity. To do so, we are taking advantage of novel reporter mice in which autoreactive B cells are fluorescently marked (Nur77-eGFP BAC transgenic line). Current funded projects include dissecting the distinct roles of the IgM and IgD B cell receptor isotypes in regulating immune responses by autoreactive B cells. More recent work is focused on defining how Nur77 and related orphan nuclear hormone receptors function selectively to restrain activation of chronically antigen-activated B cells. Related Web Sites ...
Researchers discover an entirely new way of antagonizing a human nuclear receptor. They expect this to have significant impact in the world of drug research. Nuclear receptors are modulatory proteins that control numerous crucial bodily functions and thus play a key role in many pathologies. A new, potentially better method has been found to impact the function of these proteins. This opens an avenue whereby drugs could be developed with a decreased susceptibility to resistance.
Abstract Recent studies indicate an important role for nuclear receptors in regulating lipid and carbohydrate metabolism, fibrosis and inflammation. Farnesoid X receptor (FXR) is a member of the nuclear hormone receptor superfamily. FXR is highly expressed in the liver, intestine, adrenal gland and kidney. The primary bile acids are the highest affinity endogenous ligands for FXR. The effects of FXR agonists in diabetic kidney disease, the main cause of end stage renal disease, however have not been determined. To identify the effect of FXR activation in modulation of diabetic nephropathy, we have treated 1) C57BL/6J mice on low fat diet or high fat diet with FXR agonists (GW4064 or cholic acid) for one week; 2) C57BLKS/J-db/db mice and their lean mates with GW4064 for one week; and 3) C57BL/6J-db/db mice and their lean mates with cholic acid for 12 weeks. We found that FXR agonists modulate renal SREBP-1 expression and lipid metabolism, as well as renal expression of profibrotic growth factors, ...
TY - JOUR. T1 - Expression profiling of nuclear receptors in the NCI60 cancer cell panel reveals receptor-drug and receptor-gene interactions. AU - Holbeck, Susan. AU - Chang, Jianjun. AU - Best, Anne M.. AU - Bookout, Angie L.. AU - Mangelsdorf, David J.. AU - Martinez, Elisabeth D.. PY - 2010/6. Y1 - 2010/6. N2 - We profiled the expression of the 48 human nuclear receptors (NRs) by quantitative RT-PCR in 51 human cancer cell lines of the NCI60 collection derived from nine different tissues. NR mRNA expression accurately classified melanoma, colon, and renal cancers, whereas lung, breast, prostate, central nervous system, and leukemia cell lines exhibited heterogeneous receptor expression. Importantly, receptor mRNA levels faithfully predicted the growth-inhibitory qualities of receptor ligands in nonendocrine tumors. Correlation analysis using NR expression profiles and drug response information across the cell line panel uncovered a number of new potential receptor-drug interactions, ...
Geick et al. (2001) discovered a complex regulatory cluster of several binding sites for the ligand-activated nuclear receptor, the PXR (NR1I2) in the 5′-upstream region of hMDR1. Three DR4 motifs [direct repeats of a AG(G/T)TCA motif with a spacer of four nucleotides between the binding motif], one DR3 motif, and one ER6 motif (everted repeat) were identified at approximately -8 kilobase pairs. Electrophoretic mobility shift assays further revealed that PXR binds as a heterodimer with the retinoid X receptor α to all DR4 motifs (Geick et al., 2001). In addition, reporter gene assays confirmed that this cluster of response elements is responsible for PXR-mediated hMDR1 induction.. PXR is a member of a superfamily of ligand-activated transcription factors, the so-called orphan nuclear receptors. It is activated not only by naturally occurring steroids, such as pregnenolone and progesterone, and synthetic glucocorticoids and antiglucocorticoids but also by a wide range of xenobiotics including ...
Orphan nuclear receptor that can act as a repressor or activator of transcription. An important repressor of nuclear receptor signaling pathways such as retinoic acid receptor, retinoid X, vitamin D3 receptor, thyroid hormone receptor and estrogen receptor pathways. May regulate gene expression during the late phase of spermatogenesis. Together with NR2C1, forms the core of the DRED (direct repeat erythroid-definitive) complex that represses embryonic and fetal globin transcription including that of GATA1. Binds to hormone response elements (HREs) consisting of two 5-AGGTCA-3 half site direct repeat consensus sequences. Plays a fundamental role in early embryonic development and embryonic stem cells. Required for normal spermatogenesis and cerebellum development. Appears to be important for neurodevelopmentally regulated behavior (By similarity). Activates transcriptional activity of LHCG. Antagonist of PPARA-mediated transactivation.
Nuclear receptors are ligand‐modulated transcription factors that act in the nucleus to regulate target gene transcription through interaction with cofactor proteins
NCOA4 - NCOA4 (untagged)-Human nuclear receptor coactivator 4 (NCOA4), transcript variant 5 available for purchase from OriGene - Your Gene Company.
Data published in: Bertrand S, Thisse B, Tavares R, Sachs L, Chaumot A, Bardet PL, Escrivà H, Duffraisse M, Marchand O, Safi R, Thisse C, Laudet V. Unexpected Novel Relational Links Uncovered by Extensive Developmental Profiling of Nuclear Receptor Expression. PLoS Genet. 2007 Nov 9;3(11):e188 ...
The adult heart is uniquely designed and equipped to provide a continuous supply of energy in the form of ATP to support persistent contractile function. This high-capacity energy transduction system is the result of a remarkable surge in mitochondrial biogenesis and maturation during the fetal-to-adult transition in cardiac development. Substantial evidence indicates that nuclear receptor signaling is integral to dynamic changes in the cardiac mitochondrial phenotype in response to developmental cues, in response to diverse postnatal physiologic conditions, and in disease states such as heart failure. A subset of cardiac-enriched nuclear receptors serve to match mitochondrial fuel preferences and capacity for ATP production with changing energy demands of the heart. In this Review, we describe the role of specific nuclear receptors and their coregulators in the dynamic control of mitochondrial biogenesis and energy metabolism in the normal and diseased heart.. ...
I think if you ever wanted to know what "gene expression" exactly is, look no further than nuclear receptors. You have receptors around your DNA nucleus in your cells that bind different things, this basically causes activation of your DNA to produce difference proteins ( polypeptides is a better word ) , thus expressing different genes ...
Expert-reviewed interactive pathway providing a current overview Nuclear Receptor Signaling and links to products from Cell Signaling Technology.
Click to launch & play an online audio visual presentation by Prof. Nancy Weigel and Dr. Neil McKenna on Nuclear receptors: transcriptional functions, part of a collection of online lectures.
NUCLEAR RECEPTORS FOR DEVELOPING NEW DRUG THERAPY By MD. HABIBUR RAHMAN, M.Pharm. Asst. Professor, Dept. of Pharmacology. Anurag Pharmacy College, Kodad, Nal…
Complete information for NRBP1 gene (Protein Coding), Nuclear Receptor Binding Protein 1, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
NRBF2 antibody [N1C2] (nuclear receptor binding factor 2) for WB. Anti-NRBF2 pAb (GTX119371) is tested in Human samples. 100% Ab-Assurance.
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