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Nuclear Receptor Coactivator 2 (0):
Recent article
Nuclear Receptor Coactivator 2
Cell Metabolism (12)5 2010
Abstract
We generated TIF2((i)skm)⁻(/)⁻ mice in which TIF2 was selectively ablated in skeletal muscle myofibers at adulthood. We found that increased mitochondrial uncoupling in skeletal muscle myocytes protected these mice from decreased muscle oxidative capacities induced by sedentariness, delayed the...
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PMID: 21035760
PDF is available here.
PDF is available here.
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Journal of Biological Chemistry (285)29 2010
Abstract
We identified genes regulated by the unliganded and liganded forms of ERalpha and ERbeta in U2OS cells. Microarray data demonstrated that virtually no gene regulation occurred with unliganded ERalpha, whereas many genes were regulated by estradiol (E(2)). These results demonstrated that ERalpha requ...
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PMID: 20404318
PDF is available here.
PDF is available here.
Abstract
We have previously identified a K303R ERalpha mutation within the hinge region of ERalpha. This mutation results in an altered posttranslational regulation and increased in vitro growth in the presence of low estrogen concentrations. We sought to determine if cells expressing this mutant ERalpha wou...
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PMID: 19842032
PDF is available here.
PDF is available here.
Abstract
Variations in the estrogenic activity of the phytoestrogen-rich plant, Pueraria mirifica, were determined with yeast estrogen screen (YES) consisting of human estrogen receptors (hER) hERalpha and hERbeta and human transcriptional intermediary factor 2 (hTIF2) or human steroid receptor coactivator 1...
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PMID: 20027484
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (284)50 2009
Abstract
We show that the interaction between AR and MAGE-11 is mediated by AR NH(2)-terminal FXXLF motif binding to a highly conserved MAGE-11 F-box in the MAGE homology domain, and is modulated by serum stimulation of mitogen-activated protein kinase phosphorylation of MAGE-11 Ser-174. The MAGE-11-dependen...
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PMID: 19828458
PDF is available here.
PDF is available here.
Abstract
The three homologous members of the p160 SRC family (SRC1, SRC2 and SRC3) mediate the transcriptional functions of nuclear receptors and other transcription factors, and are the most studied of all the transcriptional co-activators. Recent work has indicated that the SRCgenes are subject to amplific...
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PMID: 19701241
PDF is available here.
PDF is available here.
Physiological Genomics (38)2 2009
Abstract
We recently reported a novel role for Foxa2 in bile acid metabolism. The winged helix transcription factor Foxa2 is required to prevent intrahepatic cholestasis and liver injury in mice fed a cholic acid-enriched diet. Here, we use functional genomics to study how Foxa2 regulates its targets in a ch...
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PMID: 19417011
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (284)28 2009
Abstract
We examined the consequences of deletion of SRC-2 on bone using SRC-2 knock out (KO) mice. Loss of SRC-2 resulted in increased bone mass, with SRC-2 KO mice having 80% higher trabecular bone volume as compared with wild type mice. SRC-2 KO mice also had a marked decrease (by 50%) in bone marrow adip...
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PMID: 19423703
PDF is available here.
PDF is available here.
Abstract
We identified two distinct classes of VDR coactivators, VDR-interacting protein (DRIP) and steroid receptor coactivator (SRC) at different stages of keratinocyte differentiation. Here, we determined the functions of VDR and coactivators in lipid production and permeability barrier formation. Silenci...
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PMID: 19052561
PDF is available here.
PDF is available here.
Abstract
ER beta, AIB1, and TIF2 appear to be involved in colorectal tumorigenesis and might have prognostic significance....
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PMID: 19198856
PDF is available here.
PDF is available here.
Abstract
To explore the possible mechanism of the inhibitory effect of liver X receptor alpha (LXRalpha) on lipopolysaccharide (LPS)-induced inflammation in mouse Kupffer cells (KCs).
The KCs isolated from the liver of male KM mice and cultured in RPMI 1640 containing 20% FBS...
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PMID: 19460690
PDF is available here.
PDF is available here.
Abstract
We explored an association between IL-6 and bicalutamide resistance. To study this, series of lower and higher passages of LNCaP cell sublines generated by long-term exposure to IL-6 were used. The cells from higher passages of LNCaP treated with IL-6 developed resistance to bicalutamide treatment c...
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PMID: 19240160
PDF is available here.
PDF is available here.
Abstract
It was found that constitutive activation of PSA expression was the result of sustained occupancy by the AR at the regulatory region of this gene. This stable AR loading was not blocked by the AR antagonist bicalutamide. Furthermore, androgen-resistant CaP cells highly expressed both AR and the p160...
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PMID: 18780293
PDF is available here.
PDF is available here.
Abstract
We have identified the transcriptional coactivator SRC-2 as a regulator of fasting hepatic glucose release, a function that SRC-2 performs by controlling the expression of hepatic G6Pase. SRC-2 modulates G6Pase expression directly by acting as a coactivator with the orphan nuclear receptor RORalpha....
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PMID: 19039140
PDF is available here.
PDF is available here.
Molecular and Cellular Endocrinology (295)1-2 2008
Abstract
We have examined the effects on GR-mediated repression of five modulators (coactivators TIF2 [GRIP1, SRC-2] and SRC-1, corepressor SMRT, and comodulators STAMP and Ubc9), a glucocorticoid steroid (deacylcortivazol [DAC]) of very different structure, and an inhibitor of histone deacetylation (trichos...
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PMID: 18583028
PDF is available here.
PDF is available here.
Endocrinology (149)9 2008
Abstract
We demonstrate that COS-1 and MCF-7 cells treated with cAMP-elevating agents and 8-para-chlorophenylthio-cAMP for short periods of time showed an increase in GRIP1 coactivator function, whereas prolonged stimulation of the cAMP/PKA pathway led to a decline in GRIP1-mediated activation and protein le...
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PMID: 18499756
PDF is available here.
PDF is available here.
Endocrine Journal (55)4 2008
Abstract
We cloned a novel splicing variant for nuclear coactivator p120(alpha), designated as p120beta and studied its function and expression in several human prostate diseases. Transfection assays demonstrated that p120beta functions as a strong coactivator for androgen receptor (AR), but weakly for other...
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PMID: 18560202
PDF is available here.
PDF is available here.
Abstract
We cloned these three porcine genes, identified their transcript variants and analyzed their expression level in relation to intramuscular fat (IMF) content in Longissimus Dorsi (LD) muscle. Both in silico cloning and PCR amplification revealed a full length cDNA sequence of 6591bp for NCOA1 (EU3466...
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PMID: 18638664
PDF is available here.
PDF is available here.
Biochemistry (Washington) (47)29 2008
Abstract
We now report that several point mutants in the LBD have little effect on the binding of either agonist steroid. However, these same mutations dramatically alter the A max and/or EC 50 of exogenous and endogenous genes in a manner that depends on steroid structure. In some cases, Dex is no longer a...
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PMID: 18578507
PDF is available here.
PDF is available here.
Molecular Endocrinology (22)7 2008
Abstract
We demonstrate that TIEG is rapidly induced in response to estrogen in osteoblasts by ERbeta, but not ERalpha. We have identified the regulatory elements utilized by ERbeta and have demonstrated that ERbeta recruits steroid receptor coactivator (SRC)1 and SRC2 to this regulatory region. Additionally...
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PMID: 18483178
PDF is available here.
PDF is available here.
Abstract
An X-ray crystal structure is reported for the novel enhanced-affinity glucocorticoid agonist fluticasone furoate (FF) in the ligand binding domain of the glucocorticoid receptor. Comparison of this structure with those of dexamethasone and fluticasone propionate shows the 17 alpha furoate ester to...
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PMID: 18522385
PDF is available here.
PDF is available here.
PLoS Genetics (4)6 2008
Abstract
We investigated its molecular interaction with a master regulator of insulin signaling/glucose metabolism, the PPARgamma, in vitro and in high-fat diet (HFD)-fed ERbeta -/- mice (betaERKO) mice. Our in vitro experiments showed that ERbeta inhibits ligand-mediated PPARgamma-transcriptional activity....
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PMID: 18584035
PDF is available here.
PDF is available here.
Experimental Hematology (36)5 2008
Abstract
We show that tif2 is involved in embryogenesis and in primitive hematopoiesis. tif2-knockdown zebrafish embryos are smaller than controls, they demonstrate shorter tails, they display notochord deformation and they exhibit U-shaped tail somites. A synthetic RNA encoding human TIF2 rescues the tif2-k...
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PMID: 18295965
PDF is available here.
PDF is available here.
Nucleic Acids Research (36)6 2008
Abstract
We had identified the PAS-B domain of NCoA-1 as an LXXLL motif binding domain. Here we show that NCoA family members are able to interact with other full-length NCoA proteins via their PAS-B domain and they specifically interact with the CBP-interaction domain (CID/AD1) of NCoA-1. Peptide competitio...
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PMID: 18267973
PDF is available here.
PDF is available here.
Abstract
We report that the ligand pocket of glucocorticoid receptor (GR) can be continuously extended into the top half of the LBD by binding to deacylcortivazol (DAC), an extremely potent glucocorticoid. It has been puzzling for decades why DAC, which contains a phenylpyrazole replacement at the conserved...
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PMID: 18160712
PDF is available here.
PDF is available here.
Clinical Cancer Research (14)4 2008
Abstract
The ETV6-NCOA2 fusion may define a novel subgroup of acute leukemia with T-lymphoid and myeloid features, which is associated with a high prevalence of NOTCH1 mutations....
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PMID: 18281529
PDF is available here.
PDF is available here.
Molecular and Cellular Endocrinology (283)1-2 2008
Abstract
We explored the possibility that botanical agents used in Traditional Chinese Medicine for menopausal symptoms contain ERbeta-selective estrogens. We previously reported that an extract containing 22 herbs, MF101 has ERbeta-selective properties. In this study we isolated liquiritigenin, the most act...
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PMID: 18177995
PDF is available here.
PDF is available here.
Cancer Research (68)2 2008
Abstract
We identified a novel, atypical direct repeat (DR) element consisting of a consensus half-site (AGGTCA) at -125/-119 and a degenerated DR half-site (ATGTTA) at -99/-94 as sufficient and necessary for vegf-D transcription. The vegf-D DR element is bound and activated by the orphan receptors hepatocyt...
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PMID: 18199540
PDF is available here.
PDF is available here.
Abstract
Molecular and Cellular Endocrinology (280)1-2 2008
Abstract
We have shown that certain TR isoforms, such as TRbeta0, can bind as trimers to a subset of naturally occurring DNA elements. We report here that this trimeric mode of DNA recognition by TRbeta0 also results in an enhanced recruitment of coactivators in vitro and increased transcriptional activation...
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PMID: 18006144
PDF is available here.
PDF is available here.
Anticancer Research (28)1B 2008
Abstract
Increased gene and protein AR expression was not correlated with any of the clinical outcome measures. A non-monotonic correlation was observed between SRC1 and overall survival, as well as Her2/neu and time to prostate-specific PSA recurrence. CONCLUSION: Although no statistically significant relat...
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PMID: 18383880
PDF is available here.
PDF is available here.
Physiology & Behavior (92)5 2007
Abstract
We used an animal model to determine the impact of AAS on the development and expression of circadian function. Beginning on day 68 gonadally intact male rats received testosterone, nandrolone, or stanozolol via constant release pellets for 60 days; gonadally intact controls received vehicle pellets...
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PMID: 17716697
PDF is available here.
PDF is available here.
Abstract
We report studies aimed at optimization of this initial hit to determine the basic parameters of the structure-activity relationships and clarify the mechanism of action. These studies provided new insights, showing that activity and TRbeta isoform selectivity is highly correlated with the structura...
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PMID: 17918822
PDF is available here.
PDF is available here.
Life Sciences (81)19-20 2007
Abstract
We found that some flavonoids inhibited an effect on estrogen action without estrogen receptor (ER) binding. Considering the report that dioxin, an aryl hydrocarbon receptor (AhR) agonist, disrupts the transcriptional activity of ER without binding to the ER, 14 flavonoids were examined for the tran...
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PMID: 17950758
PDF is available here.
PDF is available here.
Brain Research (1174) 2007
Abstract
We test the hypothesis that expression changes of the three identified SRC genes (SRC1, SRC2 and SRC3) correlate with differences in HPA axis activity during postnatal development. First, we mapped the ontogeny of the three SRCs during postnatal development in the hippocampus. We found a time- and r...
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PMID: 17854779
PDF is available here.
PDF is available here.
Abstract
We have proposed that inhibitors, which bind to nuclear receptor surfaces that mediate assembly of the receptor's binding partners, might overcome some of these limitations. The androgen receptor (AR) plays a central role in prostate cancer, but conventional inhibitors lose effectiveness as cancer t...
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PMID: 17911242
PDF is available here.
PDF is available here.
Abstract
We describe a new androgen receptor (AR)-associated coactivator, PRMT2, which belongs to the arginine methyltransferase protein family. To search for AR-interacting proteins a fragment of the AR was used in a library screen exploiting the yeast two-hybrid technique and identifying the C-terminal reg...
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PMID: 17587566
PDF is available here.
PDF is available here.
Abstract
The mutant receptor hGRalphaF737L causes generalized glucocorticoid resistance because of decreased affinity for the ligand, marked delay in nuclear translocation, and/or abnormal interaction with the glucocorticoid receptor-interacting protein 1 coactivator. These findings confirm the importance of...
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PMID: 17635946
PDF is available here.
PDF is available here.
Endocrinology (148)9 2007
Abstract
The role of the p160 steroid receptor coactivator 2 (SRC-2) in the regulation of uterine function and progesterone (P4) signaling was investigated by determining the expression pattern of SRC-2 in the murine uterus during pregnancy and the impact of SRC-2 ablation on uterine function and global uter...
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PMID: 17556502
PDF is available here.
PDF is available here.
Journal of Cell Science (120)Pt 15 2007
Abstract
We identified estrogen-related receptor gamma (ERRgamma) as a GNL3L-specific binding protein. GNL3L and ERRgamma are coexpressed in the eye, kidney and muscle, and co-reside in the nucleoplasm. The interaction between GNL3L and ERRgamma requires the intermediate domain of GNL3L and the AF2-domain of...
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PMID: 17623774
PDF is available here.
PDF is available here.
Biochemistry (Washington) (46)27 2007
Abstract
We use biochemical approaches (mammalian two-hybrid, pull-down, and coimmunoprecipitation assays) to locate an N-terminal GR region that is sufficient to bind TIF2.0. In contrast, an N-terminal sequence of PR-B that is largely missing in the shorter PR-A is necessary but not sufficient for TIF2.0 bi...
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PMID: 17571860
PDF is available here.
PDF is available here.
Abstract
In addition to the human papillomavirus (HPV)-induced immortalization of epithelial cells, which usually requires integration of the viral DNA into the host cell genome, steroid hormone-activated nuclear receptors (NRs) are thought to bind to specific DNA sequences within transcriptional regulatory...
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PMID: 17376404
PDF is available here.
PDF is available here.
Molecular Pharmacology (71)5 2007
Abstract
We investigated the effects of three 1,25(OH)(2)D(3) derivatives on VDR function. AD47 has an adamantane ring and LAC67a and LAC67b have lactone ring substituents at the side chain position. These vitamin D derivatives bind to VDR but do not stabilize an active cofactor conformation. In a VDR transf...
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PMID: 17325131
PDF is available here.
PDF is available here.
Abstract
We investigated the GR-SRCs interactions in two glial cells: astrocytes for the central nervous system and Schwann cells for the peripheral nervous system. We have shown by performing functional studies (overexpression and siRNA knock-down) that the recruitment of the three p160 by the GR is promote...
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PMID: 17481888
PDF is available here.
PDF is available here.
Abstract
Vitamin D receptor (VDR) mediates a wide variety of vitamin D actions through transcriptional controls of target genes as a ligand-dependent transcription factor. The transactivation by VDR is known to associate with two co-activator complexes, DRIP/TRAP and p160/CBP, through physical interaction wi...
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PMID: 16949543
PDF is available here.
PDF is available here.
Abstract
We developed an adenoviral system to knock down, or in the case of VDR, overexpress these genes. In order to study all stages of keratinocyte development, we employed an advanced differentiated normal human keratinocyte culture system that produces a multilayer phenotype similar to that of normal sk...
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PMID: 17082781
PDF is available here.
PDF is available here.
Journal of Biological Chemistry (282)10 2007
Abstract
We have utilized metamorphosis in Xenopus laevis to study the role of these coactivators during post-embryonic development. Metamorphosis is totally dependent on the thyroid hormone, and TR mediates a vast majority, if not all, of the developmental effects of the hormone. We have previously shown th...
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PMID: 17218308
PDF is available here.
PDF is available here.
Abstract
These results support previous observations in mammalian cells that REA does not prevent ERalpha from binding to DNA but does inhibit potentiation of ERalpha-mediated transactivation by SRC1. The results in the present study further characterize REA-mediated repression, and demonstrate the utility o...
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PMID: 17194583
PDF is available here.
PDF is available here.
Abstract
Two-photon, two-color fluorescence cross-correlation spectroscopy (TPTCFCCS) was used to directly detect ligand-dependent interaction between an eCFP-fusion of the androgen receptor (eCFP-AR) and an eYFP fusion of the nuclear receptor co-activator, Tif2 (eYFP-Tif2) in live cells. As expected, these...
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PMID: 17021805
PDF is available here.
PDF is available here.
Abstract
We describe the isolation and characterization of the predicted factor as a new 1,277-amino-acid endogenous protein (STAMP). STAMP associates with coactivators (TIF2 and SRC-1) and is selective for a subset of the steroid/nuclear receptors including GRs. Transfected STAMP increases the effects of TI...
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PMID: 17116691
PDF is available here.
PDF is available here.
Cancer Investigation (25)1 2007
Abstract
We explored the mechanisms of androgen-hypersensitivity in prostate cancer cells which may thus play a role in hormone-resistance. We examined the androgen receptor (AR) DNA sequence and the expression levels of AR and 8 AR cofactors in LNCaP and LN-TR2 cells. As a result, no novel mutation was deve...
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PMID: 17364555
PDF is available here.
PDF is available here.
Molecular and Cellular Endocrinology (263)1-2 2007
Abstract
The clinical phenotype of complete androgen insensitivity (CAIS) was associated with a mutation in the human androgen receptor (hAR) gene encoding the amino acid substitution, M745I, in the hAR protein. Transcriptional activation of hAR(M745I) by the synthetic androgen, methyltrienolone (R1881), was...
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PMID: 17011702
PDF is available here.
PDF is available here.
Abstract
The importance of the progesterone receptor (PR) in transducing the progestin signal is firmly established in female reproductive and mammary gland biology; however, the coregulators preferentially recruited by PR in these systems have yet to be comprehensively investigated. Using an...
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PMID: 18540568
PDF is available here.
PDF is available here.
Bioconjugate Chemistry (18)3 2007
Abstract
A high-throughput screening system for analyzing small molecule-induced coactivator (CoA) recruitment by the vitamin D receptor (VDR) has been developed. The vitamin D-induced protein-protein interactions between VDR and fluorophore (Cy3 or Cy5)-labeled TIF2 or SRC-1 were successfully detected by us...
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PMID: 17408240
PDF is available here.
PDF is available here.
Abstract
The importance of the progesterone receptor (PR) in female reproductive and mammary gland biology is well recognized; however, the coregulators selectively enlisted by PR have yet to be comprehensively defined in vivo. To evaluate the involvement of steroid receptor coactivator (SRC)/p160 family mem...
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PMID: 17485327
PDF is available here.
PDF is available here.
Molecular Cancer (6)1 2007
Abstract
A series of deletions from the N-terminus of the MOZ-TIF2 fusion protein demonstrated that the MOZ portion is essential for nuclear localization of the fusion protein. Transient expression of MOZ-TIF2 dramatically decreased both basal and estradiol inducible reporter gene activity in an estrogen rec...
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PMID: 17697320
PDF is available here.
PDF is available here.
Abstract
We analyzed single nucleotide polymorphisms (SNP) in the genes for the GC receptor (GR), CYP3A4, cAMP-responsive element binding protein-binding protein (CBP), and nuclear receptor co-activator 2 (NCoA2). Among the patients examined, A/G alleles of the CBP gene were demonstrated in 32.4% of those wi...
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PMID: 17704997
PDF is available here.
PDF is available here.
Nucleic Acids Research (35)7 2007
Abstract
Orphan nuclear receptor TR2 is a preadipocyte proliferator. Knockdown of TR2 in 3T3-L1 preadipocytes reduced their proliferation efficiency, whereas specific elevation of TR2 in these cells facilitated their proliferation. All-trans retinoic acid (RA) stimulates cellular proliferation in 3T3-L1 prea...
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PMID: 17389641
PDF is available here.
PDF is available here.
Abstract
The peroxisome proliferator-activated receptor gamma (PPARgamma) regulates adipocyte differentiation and glucose homeostasis and is the molecular target of thiazolidinediones (TZDs) that act as insulin-sensitizers in patients with type 2 diabetes. PPARgamma is also expressed in macro...
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PMID: 18269183
PDF is available here.
PDF is available here.
Abstract
Although the importance of the progesterone receptor (PR) to female reproductive and mammary gland biology is firmly established, the coregulators selectively co-opted by PR in these systems have not been clearly delineated. A selective gene-knockout approach applied to the mouse, which abrogates ge...
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PMID: 18174919
PDF is available here.
PDF is available here.